Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
1185 3645 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3645 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3645 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3645 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
1185 3645 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 3645 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 3645 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 3645 32 None -5 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
53386917 63189 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 63189 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53388960 63237 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800663 63237 0 None - 1 Human 10.2 pIC50 = 10.2 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
11512905 137890 0 None 1778 2 Human 10.2 pIC50 = 10.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 137890 0 None 1778 2 Human 10.2 pIC50 = 10.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
9961721 167914 0 None 60 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 167914 0 None 60 2 Human 10.2 pIC50 = 10.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
53388958 63235 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800661 63235 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
18324807 63242 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 63242 0 None - 1 Human 10.1 pIC50 = 10.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
20691661 79203 0 None 138 2 Human 10.0 pIC50 = 10 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 79203 0 None 138 2 Human 10.0 pIC50 = 10 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
10100930 63188 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 63188 0 None - 1 Human 9.8 pIC50 = 9.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386915 63186 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 63186 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53389117 63240 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800666 63240 0 None - 1 Human 9.7 pIC50 = 9.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389115 63238 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800664 63238 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53387071 63190 4 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 63190 4 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10371708 63191 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 63191 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389118 63241 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800667 63241 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53386756 63243 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800669 63243 0 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44293301 187921 0 None - 1 Rat 9.5 pIC50 = 9.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50283 187921 0 None - 1 Rat 9.5 pIC50 = 9.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
16221494 161403 0 None 8 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL415659 161403 0 None 8 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
10348973 3261 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3261 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3261 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3261 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3261 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
53386757 63244 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
CHEMBL1800670 63244 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
10100930 63188 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 63188 0 None - 1 Human 9.4 pIC50 = 9.4 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386917 63189 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 63189 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
11421412 178164 11 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL468551 178164 11 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11477988 90579 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 90579 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
16155709 167910 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL435141 167910 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155709 167910 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL435141 167910 0 None - 1 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1661 42 17 19 1.7 CONC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL262747 208801 8 None 1 2 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
101755083 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
16136245 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
4379 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
5585 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
CHEMBL415606 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
DB06699 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
101755083 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
16136245 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
4379 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
5585 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
CHEMBL415606 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
DB06699 1332 42 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None None 10.1021/jm060240a
44293163 188115 0 None - 1 Rat 9.2 pIC50 = 9.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 188115 0 None - 1 Rat 9.2 pIC50 = 9.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL407661 210928 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
11262242 188152 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL505033 188152 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
16221267 141470 0 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL387499 141470 0 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
23656390 161134 0 None 4 2 Rat 9.2 pIC50 = 9.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL413245 161134 0 None 4 2 Rat 9.2 pIC50 = 9.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
1184 3676 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptorInhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 3676 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptorInhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 3676 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptorInhibition of LHRH-stimulated arachidonic acid (AA) release from CHO cells expressing human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
1184 3676 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 3676 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 3676 31 None 2 2 Human 9.2 pIC50 = 9.2 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing human LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL407661 210928 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL262747 208801 8 None 1 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL262747 208801 8 None 1 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL434380 211906 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@@H](C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)cc1 10.1021/jm060240a
44395623 124137 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL364167 124137 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL434380 211906 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@@H](C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)cc1 10.1021/jm060240a
16221104 85133 0 None 6 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL227861 85133 0 None 6 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
87285768 169927 1 None 158 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169927 1 None 158 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
22129998 100805 0 None - 1 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 100805 0 None - 1 Rat 9.1 pIC50 = 9.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
16156699 166013 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL427976 166013 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16221266 165806 0 None 2 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL427438 165806 0 None 2 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
44395435 123295 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362371 123295 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
16221495 85098 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL227451 85098 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
16156699 166013 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL427976 166013 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1647 41 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
10348973 3261 50 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3261 50 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3261 50 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3261 50 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3261 50 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
9895596 63185 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 63185 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
16221556 167786 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
CHEMBL434371 167786 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
CHEMBL429527 211788 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
155531714 175617 0 None 501 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175617 0 None 501 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assayAntagonist activity against human GnRH receptor expressed in human Chem1 cells assessed as inhibition of LHRH-induced calcium flux by FLIPR assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL429527 211788 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NO)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16221496 142215 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
CHEMBL389248 142215 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1580 41 14 17 2.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C(N)=O)[S+](C)[O-])cc1 10.1021/jm0613931
16156573 168310 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL438239 168310 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16156573 168310 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL438239 168310 0 None - 1 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1747 48 17 20 2.2 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
10649568 14397 0 None 4 2 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL120432 14397 0 None 4 2 Human 9.1 pIC50 = 9.1 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL219061 207659 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL219061 207659 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
53387071 63190 4 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 63190 4 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10371708 63191 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 63191 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
10649568 14397 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Activity at human GnRH receptor by inositol phosphate functional assayActivity at human GnRH receptor by inositol phosphate functional assay
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm701249f
CHEMBL120432 14397 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Activity at human GnRH receptor by inositol phosphate functional assayActivity at human GnRH receptor by inositol phosphate functional assay
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm701249f
53386916 63187 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800154 63187 0 None - 1 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation countingAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10649568 14397 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Functional antagonism at the human GnRH receptor (PI turnover)Functional antagonism at the human GnRH receptor (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14397 0 None 4 2 Human 9.0 pIC50 = 9 Functional
Functional antagonism at the human GnRH receptor (PI turnover)Functional antagonism at the human GnRH receptor (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44321052 204548 0 None - 1 Human 9.0 pIC50 = 9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86912 204548 0 None - 1 Human 9.0 pIC50 = 9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
16155593 157891 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409044 157891 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155593 157891 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409044 157891 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1767 53 17 21 2.2 CONC(=O)NCCOCCOCCOCCC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409043 210996 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL409043 210996 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16221433 141631 0 None 1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL388369 141631 0 None 1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
16221211 168696 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL441211 168696 0 None 2 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
44432651 86276 0 None 21 2 Rat 8.9 pIC50 = 8.9 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231760 86276 0 None 21 2 Rat 8.9 pIC50 = 8.9 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
53386915 63186 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 63186 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44395650 168755 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL441676 168755 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL2105773 210994 7 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL409018 210994 7 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
16155157 96001 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL262180 96001 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398152 159668 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 42 17 20 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL410967 159668 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 42 17 20 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16155157 96001 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL262180 96001 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1622 44 16 18 3.6 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL2105773 210994 7 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL409018 210994 7 None -1 2 Human 8.9 pIC50 = 8.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
18324807 63242 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 63242 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL2105773 210994 7 None 1 2 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL409018 210994 7 None 1 2 Rat 8.9 pIC50 = 8.9 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
44321964 95972 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL261979 95972 0 None - 1 Human 8.9 pIC50 = 8.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
16156328 96204 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL263691 96204 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398047 96465 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL265879 96465 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16156328 96204 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL263691 96204 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1592 43 16 17 3.4 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376654 210506 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376654 210506 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398065 155172 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1671 41 17 18 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL405273 155172 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1671 41 17 18 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
11250647 1516 40 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
5293 1516 40 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
8362 1516 40 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
CHEMBL1208155 1516 40 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
DB11979 1516 40 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
44449120 94789 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 94789 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL262747 208801 8 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
44380487 167018 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL430069 167018 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
23656390 161134 0 None -4 2 Human 8.8 pIC50 = 8.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL413245 161134 0 None -4 2 Human 8.8 pIC50 = 8.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL219562 207672 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)CNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL219562 207672 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)CNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
44398064 166457 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1647 40 17 20 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL428825 166457 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1647 40 17 20 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
145957953 161581 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 633 9 1 9 4.3 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4161566 161581 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 633 9 1 9 4.3 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
44398063 161260 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL414347 161260 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
58239302 161441 0 None 616 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4159247 161441 0 None 616 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44395462 167660 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL433594 167660 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
16155358 137608 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376728 137608 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398043 161148 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1603 37 17 18 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL413450 161148 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1603 37 17 18 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16155358 137608 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376728 137608 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1778 49 18 21 1.9 CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
101755083 1332 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
16136245 1332 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
4379 1332 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
5585 1332 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
CHEMBL415606 1332 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
DB06699 1332 42 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None None 10.1021/jm050134t
16156341 161182 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL413688 161182 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16156341 161182 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL413688 161182 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1929 63 17 25 2.5 CONC(=O)NCCOCCOCCOCCOCCOCCOCCC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)NOC)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155098 160118 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411337 160118 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16155098 160118 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411337 160118 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1656 43 19 19 0.1 CONC(=O)NCC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16221267 141470 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL387499 141470 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
16221266 165806 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
CHEMBL427438 165806 0 None -2 2 Rat 8.8 pIC50 = 8.8 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 41 14 17 3.7 CS[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm0613931
44398150 96253 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 40 17 18 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL264090 96253 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 40 17 18 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398066 96698 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1701 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNC(C(=O)O)C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL267873 96698 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1701 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCNC(C(=O)O)C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398045 161417 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1715 40 19 20 -1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)[C@H]1CC(=O)NC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415820 161417 0 None - 1 Human 8.8 pIC50 = 8.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1715 40 19 20 -1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=O)[C@H]1CC(=O)NC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44293111 100748 0 None -5 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295917 100748 0 None -5 2 Rat 8.7 pIC50 = 8.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44398151 161401 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1689 43 17 20 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415595 161401 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1689 43 17 20 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398046 160779 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N(C)[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL412500 160779 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N(C)[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
1185 3645 32 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3645 32 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3645 32 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3645 32 None -5 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
44320921 106685 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316362 106685 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44398135 96356 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 41 16 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CN(C)CCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL265020 96356 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1675 41 16 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CN(C)CCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44398001 168389 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL438905 168389 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1661 41 17 20 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CNCCC(=O)OC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
10004181 100617 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL294910 100617 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44292974 100925 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL297238 100925 0 None - 1 Rat 8.0 pIC50 = 8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44460342 167359 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL431402 167359 0 None - 1 Human 8.0 pIC50 = 8 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
16656823 128141 0 None - 1 Human 8.0 pIC50 = 8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 468 5 2 6 4.3 CC(C)(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
CHEMBL3668011 128141 0 None - 1 Human 8.0 pIC50 = 8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 468 5 2 6 4.3 CC(C)(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
11191675 63052 0 None - 1 Human 8.0 pIC50 = 8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 63052 0 None - 1 Human 8.0 pIC50 = 8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 63052 0 None - 1 Human 8.0 pIC50 = 8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
1185 3645 32 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 3645 32 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 3645 32 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 3645 32 None -5 2 Human 8.0 pIC50 = 8 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
44380317 167924 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL435262 167924 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
44359191 12100 0 None 173 2 Human 8.0 pIC50 = 8.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184298 12100 0 None 173 2 Human 8.0 pIC50 = 8.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL343396 12100 0 None 173 2 Human 8.0 pIC50 = 8.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44398121 96185 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1655 41 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
77232195 96185 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1655 41 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL263507 96185 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1655 41 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16145131 158933 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cc(O)nc(O)n3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361540 158933 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cc(O)nc(O)n3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL410165 158933 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cc(O)nc(O)n3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361888 141244 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL386105 141244 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL2369138 207852 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44380222 57291 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166778 57291 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293010 173675 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 472 7 2 8 5.0 O=[N+]([O-])c1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45490 173675 0 None - 1 Rat 7.0 pIC50 = 7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 472 7 2 8 5.0 O=[N+]([O-])c1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
1179 947 31 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
9957278 947 31 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
CHEMBL494803 947 31 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
44434414 88098 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
CHEMBL235179 88098 0 None - 1 Human 6.0 pIC50 = 6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
44293594 101096 0 None -10 2 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298497 101096 0 None -10 2 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293349 183542 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48273 183542 0 None - 1 Rat 6.0 pIC50 = 6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
145993478 166766 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
CHEMBL4294163 166766 0 None - 1 Human 5.0 pIC50 = 5 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
44577102 177951 0 None - 1 Human 5.0 pIC50 = 5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 303 5 1 4 4.1 CCSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1021/jm701249f
CHEMBL466735 177951 0 None - 1 Human 5.0 pIC50 = 5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 303 5 1 4 4.1 CCSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1021/jm701249f
118098039 128135 0 None - 1 Human 7.0 pIC50 = 7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 461 4 1 6 3.5 Cc1cccc(N(C)S(=O)(=O)c2ccc(Cl)c(-n3c(=O)[nH]c4sccc4c3=O)c2)c1 nan
CHEMBL3668005 128135 0 None - 1 Human 7.0 pIC50 = 7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 461 4 1 6 3.5 Cc1cccc(N(C)S(=O)(=O)c2ccc(Cl)c(-n3c(=O)[nH]c4sccc4c3=O)c2)c1 nan
44380681 58466 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168726 58466 0 None - 1 Human 7.0 pIC50 = 7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44341198 112559 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL331144 112559 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
145959547 161733 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1ccccc1C(N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4164102 161733 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1ccccc1C(N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
44359191 12100 0 None -173 2 Rat 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184298 12100 0 None -173 2 Rat 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL343396 12100 0 None -173 2 Rat 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
11467552 172142 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL450471 172142 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44561397 189232 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 189232 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44341197 108548 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL321258 108548 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
44321394 106456 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
CHEMBL314860 106456 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
44395677 66405 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185738 66405 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44380538 58776 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169620 58776 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380318 119873 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353308 119873 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
44293151 100705 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
CHEMBL295595 100705 0 None 23 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
44432638 86357 0 None 10 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232151 86357 0 None 10 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
44451397 95458 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL259220 95458 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44444665 93767 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249772 93767 0 None -2 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44432638 86357 0 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232151 86357 0 None -10 2 Human 6.0 pIC50 = 6.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
10208964 66349 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185438 66349 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44444676 154399 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401080 154399 0 None -1 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444628 93883 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250568 93883 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
44340929 113003 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL332049 113003 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44293591 101125 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 101125 0 None 1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44572286 180219 0 None -6 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 180219 0 None -6 2 Rat 6.9 pIC50 = 6.9 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11237922 65189 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1021/jm701249f
CHEMBL183066 65189 0 None 1 2 Human 6.9 pIC50 = 6.9 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1021/jm701249f
44293194 185853 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48763 185853 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
44292919 100676 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 100676 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
25193798 169631 0 None 2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL444509 169631 0 None 2 2 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44293802 101562 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL301802 101562 0 None -1 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293273 161543 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL416102 161543 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293164 167268 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL430763 167268 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44321496 105483 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
CHEMBL312995 105483 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
145980339 166034 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4280124 166034 0 None - 1 Human 4.9 pIC50 = 4.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
44359333 11525 0 None -151 2 Rat 5.9 pIC50 = 5.9 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180707 11525 0 None -151 2 Rat 5.9 pIC50 = 5.9 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138999 11525 0 None -151 2 Rat 5.9 pIC50 = 5.9 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44361524 168029 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1623 40 15 17 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL435925 168029 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1623 40 15 17 3.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44444632 93884 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250569 93884 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
9895596 63185 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 63185 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
16221557 165463 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL425486 165463 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
44573276 186833 0 None 4 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493731 186833 0 None 4 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
44321100 106609 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315909 106609 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44380394 119443 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL349638 119443 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44398117 161416 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1649 43 19 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415813 161416 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1649 43 19 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44358957 12038 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184158 12038 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336039 12038 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293070 165542 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL42592 165542 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
18914248 187148 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL49542 187148 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293335 172058 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 172058 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293195 184710 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL48592 184710 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44293165 101223 0 None -7 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299392 101223 0 None -7 2 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44380212 57313 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166843 57313 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44434437 150441 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395826 150441 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44359254 11527 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL1180716 11527 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL139292 11527 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
44434412 161228 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1565 39 4 26 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL414045 161228 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1565 39 4 26 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44572236 171333 0 None 6 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 171333 0 None 6 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11496945 175901 0 None 17 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 175901 0 None 17 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
24825725 192027 0 None 7 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL521674 192027 0 None 7 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44321510 106655 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316159 106655 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
9983568 98525 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 98525 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44215053 185038 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48641 185038 0 None -1 2 Human 7.9 pIC50 = 7.9 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44359285 11522 0 None 17 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180695 11522 0 None 17 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138747 11522 0 None 17 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44572287 180221 0 None 9 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475660 180221 0 None 9 2 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44292990 100728 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL295731 100728 0 None - 1 Rat 6.9 pIC50 = 6.9 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293348 100026 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 100026 0 None 1 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293487 101163 0 None -2 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299006 101163 0 None -2 2 Rat 6.9 pIC50 = 6.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
9936150 188150 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50500 188150 0 None - 1 Rat 5.9 pIC50 = 5.9 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
145952400 162185 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2ccccc2F)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4171296 162185 0 None - 1 Human 6.9 pIC50 = 6.9 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2ccccc2F)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
145950534 162255 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2cccc(F)c2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4172405 162255 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(CC(N)c2cccc(F)c2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44293605 100704 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295591 100704 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
10209293 100732 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295791 100732 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
24825725 192027 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 192027 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
12283 2292 12 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC nan
16656889 2292 12 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC nan
CHEMBL3668014 2292 12 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC nan
16656891 128144 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 522 9 2 8 3.5 COCCOc1ccc(F)c(F)c1COc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668015 128144 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 522 9 2 8 3.5 COCCOc1ccc(F)c(F)c1COc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
10438167 100712 0 None 15 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL295641 100712 0 None 15 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
44293803 188295 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50721 188295 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
20691661 79203 0 None 138 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 79203 0 None 138 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptorInhibition of LHRH-stimulated arachidonic acid release in CHO cells expressing monkey LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
145953549 161867 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 2 9 4.0 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4166067 161867 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 2 9 4.0 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44293054 101025 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297927 101025 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292919 100676 0 None 2 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 100676 0 None 2 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
15602808 8025 0 None -5 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 8025 0 None -5 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44561368 176240 0 None -42 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 176240 0 None -42 2 Rat 5.8 pIC50 = 5.8 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44434435 88134 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1575 36 6 25 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL235361 88134 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1575 36 6 25 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44572286 180219 0 None 6 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 180219 0 None 6 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293222 175387 0 None 100 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138464 175387 0 None 100 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL45883 175387 0 None 100 2 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
9958318 89796 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 89796 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
44293348 100026 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 100026 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44432653 86277 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231761 86277 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44380146 119771 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352565 119771 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
44293062 186125 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)cc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48853 186125 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)cc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44577104 178169 0 None -7 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 178169 0 None -7 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
145973813 162473 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1cccc(C(N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4175816 162473 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 604 9 1 9 3.9 Cc1cccc(C(N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
44293053 101022 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297918 101022 0 None - 1 Rat 6.8 pIC50 = 6.8 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293803 188295 0 None -1 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50721 188295 0 None -1 2 Rat 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293651 162564 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417726 162564 0 None - 1 Rat 5.8 pIC50 = 5.8 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44432656 158612 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL409825 158612 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44444641 154430 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401212 154430 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143420 162358 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4173938 162358 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44359458 12041 0 None -15 2 Rat 6.8 pIC50 = 6.8 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184171 12041 0 None -15 2 Rat 6.8 pIC50 = 6.8 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336884 12041 0 None -15 2 Rat 6.8 pIC50 = 6.8 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
145955260 161984 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccc(F)cc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4167957 161984 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 608 9 1 9 3.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccc(F)cc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
16656887 128142 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 504 6 2 7 4.8 COc1ccc(F)cc1C(C)(C)Sc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668012 128142 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 504 6 2 7 4.8 COc1ccc(F)cc1C(C)(C)Sc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
44380551 58450 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168649 58450 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
145955571 162109 0 None -131 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169891 162109 0 None -131 2 Rat 6.8 pIC50 = 6.8 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
44293555 100740 0 None -141 2 Human 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295897 100740 0 None -141 2 Human 6.8 pIC50 = 6.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44444649 154466 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401418 154466 0 None -2 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44398149 160747 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1621 40 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL412212 160747 0 None - 1 Human 6.8 pIC50 = 6.8 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1621 40 18 19 0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CS)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44293041 100870 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL296819 100870 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
44292833 101070 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 480 7 2 7 5.5 Cc1cc(CC#N)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL298278 101070 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 480 7 2 7 5.5 Cc1cc(CC#N)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44292733 176209 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 548 7 4 5 6.8 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
CHEMBL46060 176209 0 None - 1 Rat 7.8 pIC50 = 7.8 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 548 7 4 5 6.8 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
10348973 3261 50 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3261 50 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3261 50 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3261 50 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3261 50 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
44577104 178169 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 178169 0 None 7 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44293249 184861 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL48616 184861 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
10077523 122199 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL360429 122199 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44395463 126254 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL365366 126254 0 None - 1 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44215055 100820 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296442 100820 0 None -1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293249 184861 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48616 184861 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
21899433 154164 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399772 154164 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44341081 167501 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL432450 167501 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
16656822 128140 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 455 4 2 6 3.4 CN(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
CHEMBL3668010 128140 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 455 4 2 6 3.4 CN(C(=O)c1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1)c1ccccc1 nan
44359333 11525 0 None 151 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180707 11525 0 None 151 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138999 11525 0 None 151 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293347 162561 0 None 4 2 Rat 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417720 162561 0 None 4 2 Rat 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293592 162340 0 None -4 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 162340 0 None -4 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44434434 147541 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1531 33 6 24 8.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL393486 147541 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1531 33 6 24 8.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434392 168432 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1389 27 4 22 9.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL439200 168432 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1389 27 4 22 9.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44444652 94066 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251578 94066 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44293111 100748 0 None -5 2 Rat 5.7 pIC50 = 5.7 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295917 100748 0 None -5 2 Rat 5.7 pIC50 = 5.7 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44444642 93934 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250770 93934 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
58022100 128133 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2ccsc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
CHEMBL3668003 128133 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2ccsc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
138978203 166147 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
CHEMBL4282476 166147 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
145984647 165863 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4277116 165863 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
138978207 166600 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
CHEMBL4290761 166600 0 None - 1 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
16657781 128136 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 517 4 2 7 3.2 O=C(O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
CHEMBL3668006 128136 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 517 4 2 7 3.2 O=C(O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
44380798 59014 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170606 59014 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380537 96113 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL263004 96113 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL2371821 208384 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CN[C@H](C(=O)O)C1CCCCC1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL438629 212035 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL438629 212035 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL2371822 208385 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL None None None C#C[C@H](NC(=O)[C@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16156049 96335 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL264781 96335 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16156049 96335 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL264781 96335 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1689 44 17 19 2.5 CCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
102090748 161258 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
16138575 161258 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL414344 161258 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
44395491 123332 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362544 123332 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10053165 183417 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL48192 183417 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44398044 154692 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 38 17 18 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL402683 154692 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1617 38 17 18 0.3 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)NC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16221433 141631 0 None -1 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL388369 141631 0 None -1 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
16221494 161403 0 None -8 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL415659 161403 0 None -8 2 Rat 8.6 pIC50 = 8.6 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
9873212 57272 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166649 57272 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
10008768 58426 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168563 58426 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL268450 209010 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL268450 209010 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@H](Cc2ccc(NC(=O)NCCOCCOCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
11365653 173618 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL454774 173618 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44448991 154802 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154802 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154802 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44320895 163710 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL421160 163710 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
44380626 58419 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168539 58419 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
16155654 165525 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL425813 165525 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16155654 165525 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL425813 165525 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 20 19 -0.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CCNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398178 161280 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 43 18 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL414507 161280 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 43 18 19 1.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44361795 167933 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL435322 167933 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL269711 209056 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
21036877 173078 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL453441 173078 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
11167850 2701 22 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1178 2701 22 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1187 2701 22 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL179691 2701 22 None - 1 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
44321101 96400 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265288 96400 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
9960399 50271 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL157412 50271 0 None - 1 Human 8.6 pIC50 = 8.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44398040 168246 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1681 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL437672 168246 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1681 41 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL264779 208885 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL268813 209020 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL264779 208885 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CONC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NOC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL268813 209020 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44293195 184710 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL48592 184710 0 None - 1 Rat 7.7 pIC50 = 7.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
15602804 7998 0 None 70 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 7998 0 None 70 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44340928 9652 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113432 9652 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
16656888 128143 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 488 5 2 7 3.3 CC(C)(c1ccccc1)S(=O)(=O)c1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668013 128143 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 488 5 2 7 3.3 CC(C)(c1ccccc1)S(=O)(=O)c1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
44293058 101523 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 483 6 2 6 6.4 CC(C)(C)c1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1 10.1016/s0960-894x(00)00318-8
CHEMBL301552 101523 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 483 6 2 6 6.4 CC(C)(C)c1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1 10.1016/s0960-894x(00)00318-8
24825725 192027 0 None -7 2 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 192027 0 None -7 2 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44293484 96268 0 None -64 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL264193 96268 0 None -64 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
44214069 100848 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL296644 100848 0 None - 1 Rat 5.7 pIC50 = 5.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
16221614 136025 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
CHEMBL373725 136025 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
44432646 146701 0 None 2 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392843 146701 0 None 2 2 Human 6.7 pIC50 = 6.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44444639 154428 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401193 154428 0 None -1 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
44321498 204582 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87099 204582 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44359471 12092 0 None 67 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184266 12092 0 None 67 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341717 12092 0 None 67 2 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44444672 168836 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL442283 168836 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
44293074 187200 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49578 187200 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44561108 185848 0 None 4 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL487627 185848 0 None 4 2 Human 4.7 pIC50 = 4.7 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44444670 94043 0 None -6 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251388 94043 0 None -6 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444673 93847 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL250389 93847 0 None -2 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
145954439 162106 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 622 9 1 9 4.0 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169864 162106 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 622 9 1 9 4.0 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4cccc([N+](=O)[O-])c4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
44341046 9981 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL115365 9981 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44359301 11531 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180754 11531 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141221 11531 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293488 101084 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL298366 101084 0 None 1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293335 172058 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 172058 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44432657 148935 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394613 148935 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44398396 161374 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1737 44 17 20 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCN(c1ccccn1)c1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415328 161374 0 None - 1 Human 7.7 pIC50 = 7.7 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1737 44 17 20 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCN(c1ccccn1)c1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
9845762 186244 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccs3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48938 186244 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccs3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44444675 154184 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399857 154184 0 None -3 2 Human 6.7 pIC50 = 6.7 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
44321497 97642 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL273390 97642 0 None - 1 Human 6.7 pIC50 = 6.7 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44293076 101351 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300268 101351 0 None - 1 Rat 6.7 pIC50 = 6.7 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293222 175387 0 None -100 2 Rat 5.7 pIC50 = 5.7 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138464 175387 0 None -100 2 Rat 5.7 pIC50 = 5.7 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL45883 175387 0 None -100 2 Rat 5.7 pIC50 = 5.7 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293126 161766 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 467 6 2 7 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL416459 161766 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 467 6 2 7 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292747 187357 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 494 7 4 5 5.8 Cc1cccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49695 187357 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 494 7 4 5 5.8 Cc1cccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44587394 171906 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL448253 171906 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44573110 186611 0 None 2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL492327 186611 0 None 2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
71449058 83985 0 None -10 2 Rat 7.6 pIC50 = 7.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111955 83985 0 None -10 2 Rat 7.6 pIC50 = 7.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2219718 83985 0 None -10 2 Rat 7.6 pIC50 = 7.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
25193700 172711 0 None 7 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL452547 172711 0 None 7 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44293163 188115 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 188115 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44444668 153745 0 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL398648 153745 0 None -2 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44434389 168338 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 838 21 2 14 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL438504 168338 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 838 21 2 14 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44292661 101319 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL300048 101319 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44561369 189874 0 None 15 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 189874 0 None 15 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44341082 9685 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113574 9685 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
11620431 178789 0 None -21 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 178789 0 None -21 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11496945 175901 0 None -17 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 175901 0 None -17 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
10258659 12093 0 None -46 2 Rat 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184268 12093 0 None -46 2 Rat 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341809 12093 0 None -46 2 Rat 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293208 170577 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL445848 170577 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292940 100794 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296244 100794 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293511 100816 0 None 3 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296426 100816 0 None 3 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293377 101433 0 None 2 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL300865 101433 0 None 2 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293236 174307 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL45639 174307 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
54584354 60926 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 515 7 2 6 6.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
CHEMBL1766108 60926 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 515 7 2 6 6.1 Cc1cc(C)cc(-c2cnc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@H]2CCCCN2)c1 10.1021/jm101501b
44293112 186712 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49293 186712 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
16221434 96739 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
CHEMBL268297 96739 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1548 40 13 16 4.7 CS[C@@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(C)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0613931
44593424 175559 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 175559 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44593424 175559 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 175559 0 None -4 2 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44341199 112560 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL331145 112560 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44398119 96810 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1646 41 18 19 -0.4 CNC(=O)C[C@H](NC(=O)[C@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL268829 96810 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1646 41 18 19 -0.4 CNC(=O)C[C@H](NC(=O)[C@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44359252 11526 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180715 11526 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139291 11526 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44432628 87327 0 None 13 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233762 87327 0 None 13 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
44448991 154802 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154802 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154802 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44293223 173729 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45501 173729 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44434387 152243 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 750 15 2 12 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL397360 152243 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 750 15 2 12 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44587393 172065 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL449468 172065 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assayAntagonist activity at human GnRH receptor expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis by whole cell assay
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44341164 9473 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112378 9473 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
44432651 86276 0 None -21 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231760 86276 0 None -21 2 Human 7.6 pIC50 = 7.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
15602805 8023 0 None -11 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 8023 0 None -11 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
44293376 101205 0 None 1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299301 101205 0 None 1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293594 101096 0 None 10 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298497 101096 0 None 10 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293131 188252 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50663 188252 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293650 161779 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL416470 161779 0 None - 1 Rat 5.6 pIC50 = 5.6 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44432641 166942 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL429976 166942 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
44292878 174398 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 441 6 2 6 5.4 Cc1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45661 174398 0 None - 1 Rat 7.6 pIC50 = 7.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 441 6 2 6 5.4 Cc1cccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
25156400 188272 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL506877 188272 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11214860 84347 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 84347 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
44380483 58766 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169569 58766 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
44292835 180673 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 526 10 2 7 6.2 CCN(CC)Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL47618 180673 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 526 10 2 7 6.2 CCN(CC)Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
1185 3645 32 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3645 32 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3645 32 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3645 32 None -5 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serumAntagonist activity at human GnRH receptor expressed in CHO cells assessed as inhibition of GnRH-induced arachidonic acid release using [5,6,8,9,11,12,14,15-3H]arachidonic acid preincubated for 15 mins measured after 45 mins by scintillation counting in presence of 40% human serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
18914272 169114 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL443768 169114 0 None - 1 Rat 6.6 pIC50 = 6.6 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44432640 154434 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401226 154434 0 None 1 2 Human 6.6 pIC50 = 6.6 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
16656819 128138 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 530 4 2 7 2.9 CNC(=O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
CHEMBL3668008 128138 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 530 4 2 7 2.9 CNC(=O)c1scc2[nH]c(=O)n(-c3cc(S(=O)(=O)N4CCCc5ccccc54)ccc3Cl)c(=O)c12 nan
145949496 162308 0 None -165 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4173065 162308 0 None -165 2 Rat 6.6 pIC50 = 6.6 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
11496610 4012 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 4012 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 4012 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
11496610 4012 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 4012 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 4012 11 None 8 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
44432653 86277 0 None -1 2 Rat 7.6 pIC50 = 7.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231761 86277 0 None -1 2 Rat 7.6 pIC50 = 7.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44444647 154462 0 None -1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401352 154462 0 None -1 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
44432640 154434 0 None -1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401226 154434 0 None -1 2 Rat 6.6 pIC50 = 6.6 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
25194090 188341 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL507973 188341 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44292983 100766 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL296084 100766 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 495 6 2 6 6.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44444635 154166 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399779 154166 0 None -2 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
16656821 128139 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 474 6 2 7 3.9 COc1cccc(F)c1C(C)Oc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668009 128139 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 474 6 2 7 3.9 COc1cccc(F)c1C(C)Oc1ccc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
16656892 128146 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 491 6 2 7 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1CN(C)c1c(F)cccc1F nan
CHEMBL3668017 128146 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 491 6 2 7 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1CN(C)c1c(F)cccc1F nan
44293305 100991 0 None 1 2 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL297703 100991 0 None 1 2 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
10032223 12097 0 None -81 2 Rat 6.5 pIC50 = 6.5 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184284 12097 0 None -81 2 Rat 6.5 pIC50 = 6.5 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342822 12097 0 None -81 2 Rat 6.5 pIC50 = 6.5 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
16146022 169552 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL444381 169552 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
9918188 154183 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399856 154183 0 None 1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
44444626 154344 0 None -1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL400739 154344 0 None -1 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
16221212 165778 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL427269 165778 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
145954419 162079 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 9 1 9 4.4 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4169486 162079 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 9 1 9 4.4 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
16156517 160180 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411381 160180 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL219532 207671 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16156517 160180 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL411381 160180 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1642 42 19 19 -0.3 CONC(=O)NC[C@@H](NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL219532 207671 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL None None None CCOCCOCCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
54582417 60924 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 488 6 2 5 5.8 Cc1cc(C)cc(-c2c(OCCC3CCCCN3)c3cc(-c4ccncn4)c(Cl)cc3[nH]c2=O)c1 10.1021/jm101501b
CHEMBL1766106 60924 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at GnRH receptor by GnRHAntagonist activity at GnRH receptor by GnRH
ChEMBL 488 6 2 5 5.8 Cc1cc(C)cc(-c2c(OCCC3CCCCN3)c3cc(-c4ccncn4)c(Cl)cc3[nH]c2=O)c1 10.1021/jm101501b
25156943 187853 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL502341 187853 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
16221211 168696 0 None -2 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL441211 168696 0 None -2 2 Rat 8.5 pIC50 = 8.5 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1566 40 14 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL2370890 208200 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44449681 95599 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL259906 95599 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
9872676 77826 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 77826 0 None 2 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at human recombinant GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
9893269 65964 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL184819 65964 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
16155218 166269 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL428484 166269 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16155218 166269 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL428484 166269 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1628 41 20 19 -0.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](CNC(=O)NO)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398182 161397 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1635 42 19 19 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL415549 161397 0 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1635 42 19 19 0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ncc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
1188 217 40 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
16131215 217 40 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
35 217 40 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1252 217 40 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
DB00106 217 40 None - 1 Human 8.5 pIC50 = 8.5 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1251 206919 21 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC/N=C(\NCC)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCN/C(=N/CC)NCC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44398179 161259 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1674 44 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL414346 161259 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1674 44 18 19 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNCc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44321963 105461 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
CHEMBL312864 105461 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
44380536 119885 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353395 119885 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
44293378 101423 0 None -37 2 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300792 101423 0 None -37 2 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
10985312 78336 0 None 91 2 Human 6.5 pIC50 = 6.5 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 78336 0 None 91 2 Human 6.5 pIC50 = 6.5 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44434390 151111 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 882 24 2 15 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL396385 151111 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 882 24 2 15 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44434438 145662 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL392008 145662 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44321458 105485 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313004 105485 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44380192 57146 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 57146 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44434402 146218 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1433 30 4 23 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL392433 146218 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1433 30 4 23 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
145958075 161762 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 10 1 10 3.7 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4164522 161762 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 10 1 10 3.7 COc1ccc(F)cc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
10258643 100913 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297151 100913 0 None - 1 Rat 7.5 pIC50 = 7.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44395502 165345 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL424991 165345 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44432647 86313 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231954 86313 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11496610 4012 11 None -8 2 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 4012 11 None -8 2 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 4012 11 None -8 2 Rat 6.5 pIC50 = 6.5 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
44292838 101047 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL298074 101047 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44359264 11523 0 None 11 2 Human 7.5 pIC50 = 7.5 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180700 11523 0 None 11 2 Human 7.5 pIC50 = 7.5 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138866 11523 0 None 11 2 Human 7.5 pIC50 = 7.5 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44292974 100925 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL297238 100925 0 None - 1 Rat 5.5 pIC50 = 5.5 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 544 7 4 5 7.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44380796 58891 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170159 58891 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
44293804 101329 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Compound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsCompound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300095 101329 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Compound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsCompound tested for the inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44214098 100824 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296483 100824 0 None - 1 Rat 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
15602807 8136 0 None -8 2 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 8136 0 None -8 2 Rat 5.5 pIC50 = 5.5 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44561141 192897 0 None 37 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL527422 192897 0 None 37 2 Human 5.5 pIC50 = 5.5 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44577069 178139 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccccc3OC)ccc2n1Cc1ccccc1 10.1021/jm701249f
CHEMBL468348 178139 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccccc3OC)ccc2n1Cc1ccccc1 10.1021/jm701249f
44432628 87327 0 None -13 2 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233762 87327 0 None -13 2 Human 5.5 pIC50 = 5.5 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
10649568 14397 0 None 4 2 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14397 0 None 4 2 Human 6.5 pIC50 = 6.5 Functional
Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)Functional antagonism at gonadotropin-releasing hormone receptor in dog (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44293130 181310 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47791 181310 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44434411 146220 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL392434 146220 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44444678 154400 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401081 154400 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
44293085 97863 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3Cl)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL274952 97863 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3Cl)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
11496610 4012 11 None -8 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 4012 11 None -8 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 4012 11 None -8 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
44359456 12098 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184286 12098 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342908 12098 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293617 188090 0 None -23 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50380 188090 0 None -23 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293134 186818 0 None 1 2 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 186818 0 None 1 2 Rat 5.4 pIC50 = 5.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44434388 89374 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 794 18 2 13 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL237729 89374 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 794 18 2 13 5.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44341186 9949 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL115192 9949 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
22129998 100805 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 100805 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
11477970 89069 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 89069 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44293377 101433 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL300865 101433 0 None -2 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293802 101562 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL301802 101562 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
145957253 161645 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 737 14 2 10 4.9 COc1ccc(F)cc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
CHEMBL4162619 161645 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 737 14 2 10 4.9 COc1ccc(F)cc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
44292888 174206 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45614 174206 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292918 170849 0 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 170849 0 None 1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44215908 93794 0 None -4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249982 93794 0 None -4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
16221329 136024 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
CHEMBL373724 136024 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1562 41 15 18 0.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)S(=O)(=O)C(C)C)cc1 10.1021/jm0613931
44449120 94789 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 94789 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
16221613 166441 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL428795 166441 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
15602808 8025 0 None 5 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 8025 0 None 5 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44321146 105924 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313946 105924 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44593425 176191 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 176191 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
44593425 176191 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
CHEMBL460480 176191 0 None 12 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
44321410 106525 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315325 106525 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321393 204547 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86911 204547 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
11226531 99059 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 99059 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
10985312 78336 0 None 91 2 Human 8.4 pIC50 = 8.4 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 78336 0 None 91 2 Human 8.4 pIC50 = 8.4 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in HumanTested for inhibition of arachidonic acid(AA) release from CHO cells in Human
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
16156639 137484 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376466 137484 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16156639 137484 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL376466 137484 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1648 47 16 17 5.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
1190 869 41 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
25074887 869 41 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
583 869 41 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1200490 869 41 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
DB00050 869 41 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
44398180 155486 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1696 42 18 19 2.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL406225 155486 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1696 42 18 19 2.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16147767 96910 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL269516 96910 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16221104 85133 0 None -6 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL227861 85133 0 None -6 2 Rat 8.4 pIC50 = 8.4 Functional
Antagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at rat GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1550 40 14 17 3.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)Sc2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
44380625 58418 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168538 58418 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
9894997 119808 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352806 119808 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
16155412 160618 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL411749 160618 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16155412 160618 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
CHEMBL411749 160618 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1864 55 18 22 2.4 CCOCCOCCNC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)NCCOCCOCC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm060240a
16221150 161386 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL415432 161386 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
9938925 57287 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166763 57287 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44380478 58447 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168637 58447 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
145955571 162109 0 None 131 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169891 162109 0 None 131 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
11331001 188435 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL509075 188435 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
16156572 166560 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL429016 166560 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
22130002 176128 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 505 6 2 6 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL45990 176128 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 505 6 2 6 5.8 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292829 176305 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 471 7 2 7 5.4 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL46157 176305 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 471 7 2 7 5.4 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
44292621 176440 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL46288 176440 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 461 6 2 6 5.7 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
9959121 187775 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50120 187775 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
21254089 181075 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47761 181075 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293376 101205 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299301 101205 0 None -1 2 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44292984 176827 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c(C)c1 10.1016/s0960-894x(00)00318-8
CHEMBL46383 176827 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 455 6 2 6 5.7 Cc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c(C)c1 10.1016/s0960-894x(00)00318-8
11583756 189062 0 None 31 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL515123 189062 0 None 31 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
21254068 101318 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300045 101318 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293488 101084 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL298366 101084 0 None -1 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293592 162340 0 None 4 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 162340 0 None 4 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293148 186903 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49412 186903 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
11532637 7633 0 None 4 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 7633 0 None 4 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44561397 189232 0 None -4 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 189232 0 None -4 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44292608 177814 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 427 6 2 6 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL46550 177814 0 None - 1 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 427 6 2 6 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccccc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44577103 178168 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 530 10 4 9 4.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(O)NC)c21 10.1021/jm701249f
CHEMBL468564 178168 0 None - 1 Human 4.4 pIC50 = 4.4 Functional
Binding affinity at human GnRH receptor by calcium mobilization assayBinding affinity at human GnRH receptor by calcium mobilization assay
ChEMBL 530 10 4 9 4.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(O)NC)c21 10.1021/jm701249f
44432645 86774 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232752 86774 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
16048665 128145 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1COc1c(OC)ccc(F)c1F nan
CHEMBL3668016 128145 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 508 7 2 8 3.5 COc1cc(F)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)cc1COc1c(OC)ccc(F)c1F nan
18914263 96453 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL265774 96453 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
11532637 7633 0 None -4 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 7633 0 None -4 2 Rat 6.4 pIC50 = 6.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44380192 57146 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 57146 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
11634198 186783 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL493344 186783 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44380624 58826 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169873 58826 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293274 100786 0 None -9 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296199 100786 0 None -9 2 Rat 6.4 pIC50 = 6.4 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
11604354 186941 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
CHEMBL494400 186941 0 None 1 2 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
44572235 188917 0 None -5 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 188917 0 None -5 2 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
44359458 12041 0 None 15 2 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184171 12041 0 None 15 2 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336884 12041 0 None 15 2 Human 7.4 pIC50 = 7.4 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44432654 159248 0 None -6 2 Rat 7.4 pIC50 = 7.4 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL410547 159248 0 None -6 2 Rat 7.4 pIC50 = 7.4 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451342 96018 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262334 96018 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
15602804 7998 0 None -70 2 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 7998 0 None -70 2 Rat 5.4 pIC50 = 5.4 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44444630 154285 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL400390 154285 0 None -3 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
44293101 186535 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 513 8 2 8 5.5 CC(=O)OCc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49162 186535 0 None - 1 Rat 7.4 pIC50 = 7.4 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 513 8 2 8 5.5 CC(=O)OCc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
145951481 162405 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 10 1 10 3.6 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4174753 162405 0 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 10 1 10 3.6 COc1ccccc1[C@@H](N)Cn1c(=O)c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
25193797 189073 0 None 4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL515200 189073 0 None 4 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44593415 188790 0 None 20 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 188790 0 None 20 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44444617 93711 0 None -3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249372 93711 0 None -3 2 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
44380319 58442 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168615 58442 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44451319 95728 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260647 95728 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44451396 156132 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406958 156132 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
25113693 161365 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL415279 161365 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44432639 86535 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL232356 86535 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
10209293 100732 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295791 100732 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 545 7 4 6 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44434431 88083 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 909 24 3 15 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL235132 88083 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 909 24 3 15 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
11331001 188435 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL509075 188435 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate productionAntagonist activity at human GnRH receptor expressed in RBL1 cells assessed as inhibition of GnRH-stimulated inositol phosphate production
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44432642 153060 0 None 1 2 Rat 7.3 pIC50 = 7.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL398060 153060 0 None 1 2 Rat 7.3 pIC50 = 7.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44293591 101125 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 101125 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44432635 86356 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232150 86356 0 None -5 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
44341056 114036 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL333614 114036 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
44398120 155751 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 41 17 19 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(=O)N(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL406535 155751 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1660 41 17 19 -0.1 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(=O)N(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44561369 189874 0 None -15 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 189874 0 None -15 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44432646 146701 0 None -2 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392843 146701 0 None -2 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44358962 12037 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184155 12037 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL335764 12037 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44395583 123827 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL363663 123827 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL268875 209026 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
15602805 8023 0 None 11 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 8023 0 None 11 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
44295755 192519 0 None 46 2 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111956 192519 0 None 46 2 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL52278 192519 0 None 46 2 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44380513 119686 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL351836 119686 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380147 119772 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352566 119772 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
1184 3676 31 None 2 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
9874838 3676 31 None 2 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL71917 3676 31 None 2 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
16156572 166560 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL429016 166560 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1678 48 16 18 5.2 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
44398395 96532 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1751 45 17 20 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CN(Cc1ccccn1)Cc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL266444 96532 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1751 45 17 20 2.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CN(Cc1ccccn1)Cc1ccccn1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44448991 154802 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154802 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154802 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
16146554 160912 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
CHEMBL412749 160912 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
10051739 85008 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 85008 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
44398181 155141 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1710 43 18 19 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL404973 155141 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1710 43 18 19 2.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](CCNc1ccc2ccccc2n1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
16147453 96670 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL267622 96670 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
9808288 110993 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL327704 110993 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11421518 164744 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 164744 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
9808288 110993 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL327704 110993 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
44361796 82979 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL219461 82979 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44395533 66465 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185986 66465 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44380148 119805 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352782 119805 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
9985901 109964 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL324654 109964 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
71449058 83985 0 None 10 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111955 83985 0 None 10 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2219718 83985 0 None 10 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
145991962 166279 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4285058 166279 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
44292988 181859 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47862 181859 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293411 188182 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50552 188182 0 None - 1 Rat 5.3 pIC50 = 5.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44359287 11530 0 None -38 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180743 11530 0 None -38 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139993 11530 0 None -38 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293163 188115 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 188115 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44398086 96588 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL266893 96588 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1645 41 16 18 1.9 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44451379 168414 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL439076 168414 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44359471 12092 0 None -67 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184266 12092 0 None -67 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341717 12092 0 None -67 2 Rat 6.3 pIC50 = 6.3 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44434428 146221 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 865 21 3 14 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL392435 146221 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 865 21 3 14 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44292606 101074 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 445 6 2 6 5.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL298300 101074 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 445 6 2 6 5.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cccc(F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292862 181065 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 477 6 2 6 6.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL47758 181065 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 477 6 2 6 6.2 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44293486 186834 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL49374 186834 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44572287 180221 0 None -9 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475660 180221 0 None -9 2 Rat 6.3 pIC50 = 6.3 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293366 161662 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL416285 161662 0 None - 1 Rat 6.3 pIC50 = 6.3 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293250 101263 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299615 101263 0 None -1 2 Rat 6.3 pIC50 = 6.3 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44432636 86957 0 None -8 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233341 86957 0 None -8 2 Human 6.3 pIC50 = 6.3 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
44460343 203634 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL79639 203634 0 None - 1 Human 7.3 pIC50 = 7.3 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44293301 187921 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50283 187921 0 None - 1 Rat 7.3 pIC50 = 7.3 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44432643 146234 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392446 146234 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44293274 100786 0 None 9 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296199 100786 0 None 9 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
22100905 183684 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48380 183684 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44593425 176191 0 None -12 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 176191 0 None -12 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
44293250 101263 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299615 101263 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
58239302 161441 0 None -616 2 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4159247 161441 0 None -616 2 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at rat GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11583756 189062 0 None -31 2 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL515123 189062 0 None -31 2 Rat 5.2 pIC50 = 5.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44359193 11533 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180764 11533 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141750 11533 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293323 100746 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295911 100746 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
22129993 178150 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 558 7 4 5 6.2 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
CHEMBL46844 178150 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 558 7 4 5 6.2 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3cccc(Br)c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
44292745 187331 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1ccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL49667 187331 0 None - 1 Rat 8.2 pIC50 = 8.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 508 7 4 5 6.1 Cc1ccc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
16144515 155586 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL406337 155586 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
11249548 98633 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 98633 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptorIn vitro inhibition of [Ca2+] influx in RBL cells expressing Gonadotropin-releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
16221328 85173 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL228197 85173 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1530 41 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](SC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
145949496 162308 0 None 165 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4173065 162308 0 None 165 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
44361802 168283 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL438018 168283 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44340906 9480 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112400 9480 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
44321291 204554 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86950 204554 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
10032223 12097 0 None 81 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184284 12097 0 None 81 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342822 12097 0 None 81 2 Human 8.2 pIC50 = 8.2 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44432652 96693 0 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL267838 96693 0 None 1 2 Rat 8.2 pIC50 = 8.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44380514 119707 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352051 119707 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL262747 208801 8 None 1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44321292 204563 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87000 204563 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44380797 58980 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170499 58980 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL2105773 210994 7 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL409018 210994 7 None -1 2 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16221151 143064 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
CHEMBL389945 143064 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1564 40 13 16 3.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)[S+](C)[O-])C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0613931
15602806 8212 0 None 7 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 8212 0 None 7 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44432648 149694 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL395225 149694 0 None 1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44292728 100767 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 487 8 2 8 5.1 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1OC 10.1016/s0960-894x(00)00318-8
CHEMBL296086 100767 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 487 8 2 8 5.1 COc1ccc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc1OC 10.1016/s0960-894x(00)00318-8
44293305 100991 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL297703 100991 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293071 101130 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL298748 101130 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293165 101223 0 None 7 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299392 101223 0 None 7 2 Human 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44341080 110089 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL325417 110089 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44293347 162561 0 None -4 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417720 162561 0 None -4 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293617 188090 0 None 23 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50380 188090 0 None 23 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44432643 146234 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392446 146234 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44293100 186683 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 485 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc(C(C)O)c1 10.1016/s0960-894x(00)00318-8
CHEMBL49276 186683 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 485 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)cc(C(C)O)c1 10.1016/s0960-894x(00)00318-8
44561368 176240 0 None 42 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 176240 0 None 42 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44432636 86957 0 None 8 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233341 86957 0 None 8 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
44432655 148954 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394634 148954 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11583756 189062 0 None 31 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL515123 189062 0 None 31 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
11712618 179646 0 None 22 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL474992 179646 0 None 22 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
25194091 188423 0 None 13 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL508898 188423 0 None 13 2 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44214108 100647 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295152 100647 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
145952498 162326 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 719 14 2 10 4.8 COc1ccccc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
CHEMBL4173316 162326 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 719 14 2 10 4.8 COc1ccccc1[C@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2F)c1=O)NCCCC(=O)O 10.1016/j.ejmech.2017.12.095
44321148 96360 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265042 96360 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321509 204468 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86431 204468 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44292874 183258 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48069 183258 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
10187208 66415 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185785 66415 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptorInhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells expressing GnRH receptor
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44434386 89378 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL237734 89378 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434391 89657 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 926 27 2 16 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL238177 89657 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 926 27 2 16 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44293015 174465 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 530 7 4 5 6.6 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
CHEMBL45675 174465 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 530 7 4 5 6.6 O=C(Nc1cc2c(OCCC3CCCCN3)c(-c3ccc4ccccc4c3)c(O)nc2cc1Cl)NC1CC1 10.1016/s0960-894x(00)00318-8
44432648 149694 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL395225 149694 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451356 95916 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL261649 95916 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
Antagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assayAntagonist activity at human recombinant GnRHR expressed in CHOK1 cells assessed as reduction in luminescence signal by luciferase reporter gene assay
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44293129 181154 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47772 181154 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
22129998 100805 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 100805 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44572236 171333 0 None -6 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 171333 0 None -6 2 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293264 100744 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295908 100744 0 None - 1 Rat 6.2 pIC50 = 6.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
16148338 161399 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL415573 161399 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10649568 14397 0 None 4 2 Human 8.2 pIC50 = 8.2 Functional
Functional antagonism at the rhesus monkey gonadotropin-releasing hormone receptorFunctional antagonism at the rhesus monkey gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14397 0 None 4 2 Human 8.2 pIC50 = 8.2 Functional
Functional antagonism at the rhesus monkey gonadotropin-releasing hormone receptorFunctional antagonism at the rhesus monkey gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44321290 204680 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87785 204680 0 None - 1 Human 8.2 pIC50 = 8.2 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44432654 159248 0 None 6 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL410547 159248 0 None 6 2 Human 8.2 pIC50 = 8.2 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
9961721 167914 0 None 60 2 Human 8.2 pIC50 = 8.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 167914 0 None 60 2 Human 8.2 pIC50 = 8.2 Functional
Tested for inhibition of arachidonic acid(AA) release from CHO cells in MonkeyTested for inhibition of arachidonic acid(AA) release from CHO cells in Monkey
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
16144832 161230 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414061 161230 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10231401 1989 1 None 1 2 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
5584 1989 1 None 1 2 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
CHEMBL314260 1989 1 None 1 2 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
44572235 188917 0 None 5 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 188917 0 None 5 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
44340888 110036 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL325091 110036 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
44380552 58451 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168655 58451 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
44380643 58410 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
CHEMBL168498 58410 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
44361468 161183 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL413698 161183 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16147757 161255 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL414266 161255 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16144824 96399 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
CHEMBL265286 96399 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
44361351 160412 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL411565 160412 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361797 161254 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414249 161254 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44293223 173729 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45501 173729 0 None - 1 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 545 8 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(CC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
9809394 120004 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL354524 120004 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293178 100952 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297430 100952 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
9809382 100208 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL292291 100208 0 None - 1 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434373 89617 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL238160 89617 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44292820 100697 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 498 8 3 7 4.4 Cc1cc(CC(N)=O)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295556 100697 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 498 8 3 7 4.4 Cc1cc(CC(N)=O)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44293011 100785 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 563 6 2 6 7.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL296198 100785 0 None - 1 Rat 7.2 pIC50 = 7.2 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 563 6 2 6 7.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44573791 186805 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493565 186805 0 None -1 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assayAntagonist activity at human recombinant GnRH receptor expressed in HEK293 cells assessed as reduction in (D-Trp6)-GnRH-stimulated IP production by whole cell assay
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44215055 100820 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296442 100820 0 None 1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293249 184861 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48616 184861 0 None -1 2 Rat 7.2 pIC50 = 7.2 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44292977 173665 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45489 173665 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44434415 88099 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 821 18 3 13 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL235180 88099 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 821 18 3 13 5.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434432 88320 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 953 27 3 16 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL236221 88320 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 953 27 3 16 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44215053 185038 0 None 1 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48641 185038 0 None 1 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293485 101045 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
CHEMBL298051 101045 0 None 2 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
44444663 93766 0 None -4 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249771 93766 0 None -4 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44593415 188790 0 None -20 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 188790 0 None -20 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44359287 11530 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180743 11530 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139993 11530 0 None 38 2 Human 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
22100905 183684 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48380 183684 0 None 1 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44359303 11532 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180760 11532 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141539 11532 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44359285 11522 0 None -17 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180695 11522 0 None -17 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138747 11522 0 None -17 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44576656 187663 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 571 10 2 7 4.2 N[C@@H](Cn1c(=O)c(-c2ccc(COCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499588 187663 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium fluxAntagonist activity at human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated calcium flux
ChEMBL 571 10 2 7 4.2 N[C@@H](Cn1c(=O)c(-c2ccc(COCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
138978204 166201 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4283577 166201 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
145992260 166381 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
CHEMBL4286937 166381 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
16147451 96566 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266653 96566 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL2370894 208201 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)C[C@@H]3NC(=O)NC3=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16147765 161302 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cnc(O)nc3O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361477 161302 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cnc(O)nc3O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414715 161302 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1628 41 16 20 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)c3cnc(O)nc3O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10051739 85008 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL22653 85008 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assayAntagonist activity at human GnRHR assessed as inhibition of calcium flux by IP3 assay
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44321345 204519 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86758 204519 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
10258659 12093 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184268 12093 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341809 12093 0 None 46 2 Human 8.1 pIC50 = 8.1 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293487 101163 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299006 101163 0 None 2 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
145973618 162535 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 635 8 1 8 4.7 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4176683 162535 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 635 8 1 8 4.7 Cc1cc(F)cc([C@@H](N)Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.ejmech.2017.12.095
44380236 58413 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168506 58413 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
16144222 96574 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266728 96574 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44341113 9828 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL114438 9828 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)Concentration required for the inhibition of phosphatidyl inositol hydrolysis in chinese hamster ovary cells expressing human GnRH receptor (Gonadotropin Release Hormone receptor)
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
44321411 106526 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315326 106526 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
101755083 1332 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
16136245 1332 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
4379 1332 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
5585 1332 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
CHEMBL415606 1332 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
DB06699 1332 42 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL None None None None 10.1021/jm0003900
44361587 160764 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
CHEMBL412336 160764 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
9872676 77826 0 None -2 2 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 77826 0 None -2 2 Rat 8.1 pIC50 = 8.1 Functional
Antagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulationAntagonist activity at rat pituitary GnRH receptor assessed as inhibition of GnRH-stimulated inositol phosphate accumulation
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
44321412 204529 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86805 204529 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
16144865 83027 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1648 43 18 18 1.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)C(NC(N)=O)NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL219799 83027 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1648 43 18 18 1.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)C(NC(N)=O)NC(N)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
53239183 162293 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 603 8 1 8 4.3 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4172886 162293 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 603 8 1 8 4.3 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
58022331 128134 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2sccc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
CHEMBL3668004 128134 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 473 3 1 6 3.5 O=c1[nH]c2sccc2c(=O)n1-c1cc(S(=O)(=O)N2CCCc3ccccc32)ccc1Cl nan
44292918 170849 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 170849 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
9936667 100052 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL291201 100052 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44432627 147596 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL393540 147596 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
10649568 14397 0 None -4 2 Rat 7.1 pIC50 = 7.1 Functional
Functional antagonism at GnRH receptor in rat (PI turnover)Functional antagonism at GnRH receptor in rat (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14397 0 None -4 2 Rat 7.1 pIC50 = 7.1 Functional
Functional antagonism at GnRH receptor in rat (PI turnover)Functional antagonism at GnRH receptor in rat (PI turnover)
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
44293177 174131 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45597 174131 0 None - 1 Rat 7.1 pIC50 = 7.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
10438167 100712 0 None -15 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL295641 100712 0 None -15 2 Rat 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
44321695 105501 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313086 105501 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
44292979 187606 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49893 187606 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
11712618 179646 0 None -22 2 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL474992 179646 0 None -22 2 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cellsAntagonist activity at rat recombinant GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated LH release from rat pituitary cells
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44293151 100705 0 None -23 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
CHEMBL295595 100705 0 None -23 2 Rat 6.1 pIC50 = 6.1 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
44560995 178574 0 None -9 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 178574 0 None -9 2 Rat 4.1 pIC50 = 4.1 Functional
Antagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH releaseAntagonist activity at recombinant GnRH receptor in CO2 asphyxiated rat primary pituitary cells assessed as reduction in (D-Trp6)LHRH-induced LH release
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44434433 88321 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 997 30 3 17 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL236222 88321 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 997 30 3 17 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCN=[N+]=[N-])nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44434436 150440 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395825 150440 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
16221379 161382 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
CHEMBL415380 161382 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assayAntagonist activity at human GnRHR expressed in HEK293 cells assessed as inhibition of GnRH-induced luciferase response by reporter gene assay
ChEMBL 1546 41 15 17 1.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](CCC(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)[S+]([O-])C(C)C)cc1 10.1021/jm0613931
58022131 128137 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 442 5 2 6 4.0 Cc1ccccc1COc1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
CHEMBL3668007 128137 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.FLIPR Calcium Assay: Antagonizing effect of compounds for human GnRHR1 was evaluated by change of calcium levels in GnRH-stimulated cells. After removing the culture medium of HEK293 cells transiently expressing human GnRHR1, cells were washed with 200 .mu.L piper well of the washing buffer (Hank's Balanced Salt Solutions, 20 mM N-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid, 1.3 mM calcium chloride, 0.5 mM magnesium chloride, 0.4 mM magnesium sulfate). One hundred .mu.L of the Ca.sup.2+sensitive dye solution (FLIPR Calcium Assay Kit (Molecular Devices)) was added to the well, and the cells were incubated for 1 hour at 37.degree. C., 5% CO.sub.2. Then, intracellular calcium levels were determined under the following condition by using FLEX STATION (Molecular Devices). In the equipment, which was warmed to 37.degree. C., 50 .mu.L of test compound diluted with the measurement buffer (the washing buffer with 0.1% Albumin bovine serum) was added to the well.
ChEMBL 442 5 2 6 4.0 Cc1ccccc1COc1ccc(Cl)c(-n2c(=O)[nH]c3csc(C(=O)O)c3c2=O)c1 nan
44432642 153060 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL398060 153060 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44432649 86272 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231739 86272 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44359264 11523 0 None -11 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180700 11523 0 None -11 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138866 11523 0 None -11 2 Rat 7.1 pIC50 = 7.1 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44185958 154459 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401349 154459 0 None -1 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
145956692 161524 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 606 9 2 10 3.3 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL4160698 161524 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells co-expressing pGL4-NFATpromoter AP-1-luc assessed as inhibition of GnRH-induced NFAT promoter activation preincubated for 1 hr followed by GnRH addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 606 9 2 10 3.3 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44380488 58707 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169238 58707 0 None - 1 Human 8.1 pIC50 = 8.1 Functional
Inhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysisInhibition of gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
44432652 96693 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL267838 96693 0 None -1 2 Human 8.1 pIC50 = 8.1 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
16146884 96722 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL268146 96722 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44398118 166744 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1632 41 18 19 -0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
CHEMBL429378 166744 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of GnRH response in HEK293 cells expressing human GnRH receptorAntagonism of GnRH response in HEK293 cells expressing human GnRH receptor
ChEMBL 1632 41 18 19 -0.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm050134t
44593424 175559 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 175559 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44593424 175559 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 175559 0 None 4 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
16156706 136577 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL374747 136577 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
16144863 96427 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL265556 96427 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cellsAntagonism of human GnHR receptor, determined in a reporter gene assay in HEK293 cells
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16156706 136577 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
CHEMBL374747 136577 0 None - 1 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assayAntagonist activity at human GnRH receptor expressed in HEK293 cells as inhibition of GnRH-induced LH secretion by reporter gene assay
ChEMBL 1745 48 17 19 4.0 CCCCCCCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)NOC)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm060240a
11620431 178789 0 None 21 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 178789 0 None 21 2 Human 8.0 pIC50 = 8.0 Functional
Antagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reductionAntagonist activity at human GnRH receptor assessed as inhibition of [D-Trp6]-GnRH-stimulated [3H]IP reduction
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
15602807 8136 0 None 8 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 8136 0 None 8 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assayAntagonist activity at human recombinant GNRH receptor assessed as inhibition of D-Trp6-GNRH-induced IP accumulation after 1 hr by rapid filtration assay
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44293485 101045 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
CHEMBL298051 101045 0 None -2 2 Human 7.1 pIC50 = 7.1 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
44292837 101002 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccsc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL297768 101002 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 433 6 2 7 5.1 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccsc3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44292683 186374 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 537 7 2 6 7.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(-c4ccccc4)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL49028 186374 0 None - 1 Rat 6.1 pIC50 = 6.1 Functional
Antagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cellsAntagonist activity against Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary cells
ChEMBL 537 7 2 6 7.4 O=[N+]([O-])c1cc2c(OCCC3CCCCN3)c(-c3ccc(-c4ccccc4)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44293134 186818 0 None -1 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 186818 0 None -1 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44432650 86344 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
CHEMBL232097 86344 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
Inhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysisInhibition of human GnRHR expressed in RBL cells assessed as inhibition of GnRH-stimulated [3H]inositol phosphate hydrolysis
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
15602806 8212 0 None -7 2 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 8212 0 None -7 2 Rat 6.0 pIC50 = 6.0 Functional
Antagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIAAntagonist activity at GNRH receptor in rat pituitary cells assessed as inhibition of D-Trp6-GnRH-induced LH accumulation after 3 hrs by RIA
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44560995 178574 0 None 9 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 178574 0 None 9 2 Human 5.0 pIC50 = 5.0 Functional
Antagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol productionAntagonist activity at human recombinant GnRH receptor assessed as reduction in (D-Trp6)LHRH-induced myo-(1,2)-[3H]inositol production
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44321147 162928 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL420051 162928 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.In vitro functional antagonism via inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned Chinese hamster ovary (CHO) cells stably expressing the human GnRH receptor.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44293443 183469 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48224 183469 0 None - 1 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293511 100816 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296426 100816 0 None -3 2 Human 7.0 pIC50 = 7.0 Functional
Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.Inhibition of GnRH-stimulated phosphatidylinositol (PI) hydrolysis in cloned chinese hamster ovary (CHO) cells expressing human GnRH receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44444645 154461 0 None -5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL401351 154461 0 None -5 2 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrsAntagonist activity at GnRH receptor expressed in AP Han Wistar rat primary pituitary cells assessed as inhibition of GnRH stimulated LH release after 24 hrs
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
44293075 90233 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL239108 90233 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292827 187605 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49891 187605 0 None - 1 Rat 7.0 pIC50 = 7.0 Functional
Inhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cellsInhibition GnRH-stimulated luteinizing hormone (LH) release from rat pituitary cells
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44434404 166015 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL427981 166015 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
Antagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assayAntagonist activity at human GnRHR expressed in CHO cells after 30 mins by luciferase reporter gene assay
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44432635 86356 0 None 5 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232150 86356 0 None 5 2 Rat 7.0 pIC50 = 7.0 Functional
Inhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH releaseInhibition of GnRHR in rat pituitary cells assessed as inhibition of GnRH-stimulated LH release
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
44295755 192519 0 None -46 2 Rat 7.0 pIC50 = 7.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111956 192519 0 None -46 2 Rat 7.0 pIC50 = 7.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL52278 192519 0 None -46 2 Rat 7.0 pIC50 = 7.0 Functional
In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.In vitro inhibition of GnRH stimulated release of luteinizing hormone from the rat primary pituitary cells.
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293486 186834 0 None 1 2 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL49374 186834 0 None 1 2 Rat 6.0 pIC50 = 6.0 Functional
Inhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cellsInhibition of GnRH-stimulated luteinizing hormone (LH) release in rat pituitary cells
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293222 175387 0 None -100 2 Rat 7.0 pIC50 = 7.0 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL138464 175387 0 None -100 2 Rat 7.0 pIC50 = 7.0 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45883 175387 0 None -100 2 Rat 7.0 pIC50 = 7.0 Functional
Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)Compound was evaluated for its antagonism in rat primary pituitary cell assay (rLH)
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44359289 12045 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL1184180 12045 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL337323 12045 0 None - 1 Human 6.0 pIC50 = 6.0 Functional
In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.In vitro inhibition of GnRH-stimulated phosphatidyl inositol hydrolysis in CHO cells stably expressing gonadotropin-releasing hormone receptor.
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
44361351 160412 0 None - 1 Human 9.5 pKd = 9.5 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL411565 160412 0 None - 1 Human 9.5 pKd = 9.5 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](Cc2ccc(CNC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16144515 155586 0 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL406337 155586 0 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1533 40 15 16 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL1251 206919 21 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC/N=C(\NCC)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCN/C(=N/CC)NCC)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL2370890 208200 0 None - 1 Human 9.3 pKd = 9.3 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](CCC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
101755083 1332 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16136245 1332 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
4379 1332 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
5585 1332 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
CHEMBL415606 1332 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
DB06699 1332 42 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16146884 96722 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL268146 96722 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.1 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CNC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361587 160764 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
CHEMBL412336 160764 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1602 41 16 17 2.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(CNC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm0003900
16146554 160912 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
CHEMBL412749 160912 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)CO 10.1021/jm0003900
44361802 168283 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL438018 168283 0 None - 1 Human 9.2 pKd = 9.2 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1547 41 15 16 2.6 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](Cc2ccc(CNC(N)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
1188 217 40 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16131215 217 40 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
35 217 40 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1252 217 40 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
DB00106 217 40 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
44361796 82979 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL219461 82979 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1583 42 17 18 0.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16147451 96566 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266653 96566 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 41 15 18 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)N(C)C(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361797 161254 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL414249 161254 0 None - 1 Human 9.1 pKd = 9.1 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1659 42 17 18 1.5 CNC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16144824 96399 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
CHEMBL265286 96399 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1632 42 17 18 1.7 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)CO 10.1021/jm0003900
16144863 96427 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL265556 96427 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16144222 96574 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL266728 96574 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
44361888 141244 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL386105 141244 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44361468 161183 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL413698 161183 0 None - 1 Human 9.0 pKd = 9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1728 42 18 20 0.6 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
1190 869 41 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
25074887 869 41 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
583 869 41 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
CHEMBL1200490 869 41 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
DB00050 869 41 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None None 10.1021/jm0003900
16147453 96670 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL267622 96670 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1645 42 17 18 1.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(CNC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
16147767 96910 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL269516 96910 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1630 41 16 18 2.0 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL268875 209026 0 None - 1 Human 8.9 pKd = 8.9 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CCNC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(=O)NCC)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
9854500 101802 0 None - 0 Rat 8.8 pKd = 8.8 Functional
Antagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cellsAntagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
CHEMBL303274 101802 0 None - 0 Rat 8.8 pKd = 8.8 Functional
Antagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cellsAntagonist activity at rat GnRH receptor assessed as luteinizing hormone release in rat pituitary cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
16148338 161399 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
CHEMBL415573 161399 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1644 42 16 18 1.7 CC(=O)NCc1ccc(C[C@@H](NC(=O)[C@H](Cc2ccc(NC(=O)[C@@H]3CC(=O)NC(=O)N3)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
16146022 169552 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL444381 169552 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1631 41 17 18 1.5 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL269711 209056 0 None - 1 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL2105773 210994 7 None -1 2 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL409018 210994 7 None -1 2 Human 8.8 pKd = 8.8 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
44361795 167933 0 None - 1 Human 8.7 pKd = 8.7 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL435322 167933 0 None - 1 Human 8.7 pKd = 8.7 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL 1574 40 15 18 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@H]2CC(=O)NC(=O)N2)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm0003900
CHEMBL262747 208801 8 None 1 2 Human 8.6 pKd = 8.6 Functional
Competitive antagonism of GnRH-induced response in the reporter gene assayCompetitive antagonism of GnRH-induced response in the reporter gene assay
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm0003900
10394119 113949 0 None - 0 Rat 8.3 pKd = 8.3 Functional
Competitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptorCompetitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 113949 0 None - 0 Rat 8.3 pKd = 8.3 Functional
Competitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptorCompetitive inhibition of GnRH-stimulated extracellular acidification in cells expressing recombinant rat GnRH receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
1184 3676 31 None 2 2 Human 10.0 pKi = 10 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
9874838 3676 31 None 2 2 Human 10.0 pKi = 10 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL71917 3676 31 None 2 2 Human 10.0 pKi = 10 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
145991962 166279 0 None - 1 Human 7.0 pKi = 7.0 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4285058 166279 0 None - 1 Human 7.0 pKi = 7.0 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 531 5 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6nc7ccccc7[nH]6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
11583756 189062 0 None 31 2 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL515123 189062 0 None 31 2 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
138978204 166201 0 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4283577 166201 0 None - 1 Human 7.9 pKi = 7.9 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 461 6 1 6 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(CCF)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
145992260 166381 0 None - 1 Human 6.8 pKi = 6.8 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
CHEMBL4286937 166381 0 None - 1 Human 6.8 pKi = 6.8 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 744 10 2 14 3.3 CC(=O)N[C@@H]1[C@@H](OC(C)=O)[C@H](OC(C)=O)[C@@H](COC(C)=O)O[C@H]1n1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1 10.1039/C7MD00320J
145993478 166766 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
CHEMBL4294163 166766 0 None - 1 Human 6.7 pKi = 6.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 602 8 3 9 4.4 CC(C)(C)OC(=O)N[C@@H](Cn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1)C(=O)O 10.1039/C7MD00320J
1179 947 31 None - 1 Human 7.7 pKi = 7.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
9957278 947 31 None - 1 Human 7.7 pKi = 7.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
CHEMBL494803 947 31 None - 1 Human 7.7 pKi = 7.7 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
145980339 166034 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4280124 166034 0 None - 1 Human 6.6 pKi = 6.6 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 380 4 1 3 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCF)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
138978203 166147 0 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
CHEMBL4282476 166147 0 None - 1 Human 7.4 pKi = 7.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 639 7 3 11 3.1 Cc1cn([C@H]2C[C@@H](n3cc(CN4CCN(c5cccc6[nH]c(-c7ccc(C(C)(C)C)cc7)nc56)CC4)nn3)[C@@H](CO)O2)c(=O)[nH]c1=O 10.1039/C7MD00320J
138978207 166600 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
CHEMBL4290761 166600 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 372 3 1 3 4.3 C#CCN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1039/C7MD00320J
145984647 165863 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
CHEMBL4277116 165863 0 None - 1 Human 6.4 pKi = 6.4 Functional
Antagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assayAntagonist activity at N-terminal FLAG-tagged human full-length GnRHR expressed in HEK293T cells assessed as inhibition of GnRH-induced calcium mobilization preincubated for 15 mins followed by agonist addition by FLIPR assay
ChEMBL 509 5 1 6 5.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cn(-c6ccc(F)cc6)nn5)CC4)cccc3[nH]2)cc1 10.1039/C7MD00320J
3860 733 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
436 733 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
50225 733 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
CHEMBL2110824 733 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
DB06719 733 0 None -2 2 Mouse 8.0 pEC50 = 8 Functional
NoneNone
Drug Central None None None None None
3860 733 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
436 733 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
50225 733 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL2110824 733 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB06719 733 0 None 2 2 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1177 3806 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
25074470 3806 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
2968 3806 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL1201334 3806 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB06825 3806 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1162 1801 0 None 16 3 Human 10.0 pEC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
16132914 1801 0 None 16 3 Human 10.0 pEC50 = 10 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
3860 733 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 733 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 733 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 733 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 733 0 None 2 2 Human 10.5 pEC50 = 10.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
1162 1801 0 None -16 3 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
16132914 1801 0 None -16 3 Mouse 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
3860 733 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 733 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 733 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 733 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 733 0 None -2 2 Mouse 9.7 pEC50 = 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
11980076 206711 27 None 1 2 Rat 8.1 pIC50 = 8.1 Functional
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
CHEMBL1007 206711 27 None 1 2 Rat 8.1 pIC50 = 8.1 Functional
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
11250647 1516 40 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
5293 1516 40 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
8362 1516 40 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
CHEMBL1208155 1516 40 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
DB11979 1516 40 None - 1 Human 8.1 pIC50 = 8.1 Functional
determined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptordetermined by competition for [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
10348973 3261 50 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5432 3261 50 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5586 3261 50 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
CHEMBL1800159 3261 50 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
DB11853 3261 50 None 1 2 Rat 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
1175 2266 38 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
1559 2266 38 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
657181 2266 38 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
CHEMBL1201199 2266 38 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
DB00007 2266 38 None 1 2 Human 8.0 pIC50 = 8.0 Functional
NoneNone
Drug Central None None None None None
10348973 3261 50 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5432 3261 50 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
5586 3261 50 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
CHEMBL1800159 3261 50 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
DB11853 3261 50 None -1 2 Human 8.0 pIC50 = 8 Functional
NoneNone
Drug Central 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC None
12784 571 8 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assayAntagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay
Guide to Pharmacology 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 32960053
85469632 571 8 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assayAntagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay
Guide to Pharmacology 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 32960053
CHEMBL4537788 571 8 None 1 3 Human 7.7 pIC50 = 7.7 Functional
Antagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assayAntagonism of buserelin-induced GnRHR activation in a proprietary IP-One HTRF assay
Guide to Pharmacology 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 32960053
12283 2292 12 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.
Guide to Pharmacology 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC 35690889
16656889 2292 12 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.
Guide to Pharmacology 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC 35690889
CHEMBL3668014 2292 12 None - 1 Human 7.4 pIC50 = 7.4 Functional
Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.Inhibition of GnRH-stimulated Ca2+ flux in HEK293 cells stably expressing hGnRHR.
Guide to Pharmacology 508 7 2 8 3.5 COc1c(c(c(cc1)F)F)COc1c(cc(c(c1)n1c(=O)c2c(scc2[nH]c1=O)C(=O)O)F)OC 35690889
11496610 4012 11 None -8 2 Rat 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
5582 4012 11 None -8 2 Rat 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
CHEMBL474991 4012 11 None -8 2 Rat 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
1164 1802 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1164 1802 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17942747
1164 1802 0 None - 1 Human 7.5 pIC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
5581 1418 0 None - 1 Human 7.6 pIC50 = 7.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
11496610 4012 11 None 8 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
5582 4012 11 None 8 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
CHEMBL474991 4012 11 None 8 2 Human 7.9 pIC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 19271735
1162 1801 0 None 16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
16132914 1801 0 None 16 3 Human 8.6 pIC50 = 8.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1190 869 41 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
25074887 869 41 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
583 869 41 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
CHEMBL1200490 869 41 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
DB00050 869 41 None - 1 Human 8.7 pIC50 = 8.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
10231401 1989 1 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
5584 1989 1 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
CHEMBL314260 1989 1 None -1 2 Rat 8.8 pIC50 = 8.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
101827019 2075 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
16130938 2075 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
3854 2075 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
73952264 2075 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
CHEMBL3989438 2075 0 None - 1 Human 9.0 pIC50 = 9.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11861490
1175 2266 38 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
1559 2266 38 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
657181 2266 38 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
CHEMBL1201199 2266 38 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
DB00007 2266 38 None -1 2 Rat 9.1 pIC50 = 9.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
5583 246 0 None - 1 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 19638591
10231401 1989 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
10231401 1989 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 12107234
5584 1989 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
5584 1989 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 12107234
CHEMBL314260 1989 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 11551758
CHEMBL314260 1989 1 None 1 2 Human 9.2 pIC50 = 9.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 12107234
10348973 3261 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
10348973 3261 50 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5432 3261 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5432 3261 50 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5586 3261 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
5586 3261 50 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
CHEMBL1800159 3261 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
CHEMBL1800159 3261 50 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
DB11853 3261 50 None -1 2 Human 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
DB11853 3261 50 None 1 2 Rat 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 21657270
12394 2455 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 752 12 2 9 6.0 C1CN(CCC21c1c(CO2)n(c(=O)n(c1=O)C[C@@H](c1ccccc1)NCCCC(=O)O)Cc1c(cccc1F)C(F)(F)F)Cc1ccc(o1)C(F)(F)F 26321528
71727383 2455 0 None - 1 Human 9.6 pIC50 = 9.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 752 12 2 9 6.0 C1CN(CCC21c1c(CO2)n(c(=O)n(c1=O)C[C@@H](c1ccccc1)NCCCC(=O)O)Cc1c(cccc1F)C(F)(F)F)Cc1ccc(o1)C(F)(F)F 26321528
1192 147 41 None -9 4 Human 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 18344315
1794 147 41 None -9 4 Human 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 18344315
CHEMBL501701 147 41 None -9 4 Human 4.3 pIC50 None 4.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 311 2 3 5 0.5 NC(=NC(=O)c1nc(Cl)c(nc1N)N1CCCCCC1)N 18344315
10279142 1596 0 None - 1 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1182 1596 0 None - 1 Human 5.3 pIC50 None 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1171 3532 0 None - 1 Human 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
118856782 3532 0 None - 1 Human 6.2 pIC50 None 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1173 3835 0 None - 1 Human 6.7 pIC50 None 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1172 3813 0 None - 1 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
16130930 3813 0 None - 1 Human 7.0 pIC50 None 7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1169 1778 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
123777 1778 0 None - 1 Human 7.1 pIC50 None 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17452338
1162 1801 0 None -39 3 Rat 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
16132914 1801 0 None -39 3 Rat 7.7 pIC50 None 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 8013367
1179 947 31 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 17176055
9957278 947 31 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 17176055
CHEMBL494803 947 31 None - 1 Human 7.8 pIC50 None 7.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 17176055
1162 1801 0 None -16 3 Mouse 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1328228
16132914 1801 0 None -16 3 Mouse 8.3 pIC50 None 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1328228
1184 3676 31 None 2 2 Human 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 9784092
9874838 3676 31 None 2 2 Human 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 9784092
CHEMBL71917 3676 31 None 2 2 Human 9.7 pIC50 None 9.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 9784092
1174 1359 0 None - 1 Mouse 9.9 pIC50 None 9.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1328228


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Ligands Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
44348326 96718 0 None - 0 Rat 10.3 pIC50 = 10.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL268095 96718 0 None - 0 Rat 10.3 pIC50 = 10.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
11563584 139018 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 630 10 2 7 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL379629 139018 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 630 10 2 7 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10100930 63188 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 63188 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53388960 63237 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800663 63237 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 682 11 2 9 6.0 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
11692959 77760 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 612 10 2 7 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210294 77760 0 None - 0 Human 10.2 pIC50 = 10.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 612 10 2 7 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(NC(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10348973 3261 50 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3261 50 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3261 50 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3261 50 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3261 50 None - 1 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
53387071 63190 4 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 63190 4 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL2370519 208122 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm010112g
53388958 63235 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800661 63235 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389117 63240 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800666 63240 0 None - 0 Human 10.1 pIC50 = 10.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 688 11 2 9 4.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN2CCCC2=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL414239 161253 0 None - 0 Rat 10.1 pIC50 = 10.1 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1530 40 18 21 -1.6 CC(C)C[C@H](NC(=O)[C@H](CCCCNC(=O)CC/N=C1\C(=O)c2ccccc2C(O)=C1Cl)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
10258719 152707 0 None - 0 Human 10.0 pIC50 = 10 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 650 12 2 10 4.8 CCOCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
CHEMBL3977463 152707 0 None - 0 Human 10.0 pIC50 = 10 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 650 12 2 10 4.8 CCOCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
1185 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
9939837 77497 0 None - 0 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 651 9 2 7 6.6 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL2092994 77497 0 None - 0 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 651 9 2 7 6.6 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9961721 167914 0 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 167914 0 None - 1 Human 10.0 pIC50 = 10 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
1185 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
3038517 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
CHEMBL22055 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
DB06494 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm701249f
44395650 168755 0 None - 0 Human 10.0 pIC50 = 10 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL441676 168755 0 None - 0 Human 10.0 pIC50 = 10 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 537 7 3 8 4.9 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
1185 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3645 32 None - 1 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
53386915 63186 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 63186 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53389115 63238 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800664 63238 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 698 11 3 10 5.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccc(CO)n2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
18324807 63242 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 63242 0 None - 0 Human 10.0 pIC50 = 10 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44293053 101022 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297918 101022 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292838 101047 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL298074 101047 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292827 187605 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49891 187605 0 None - 0 Rat 10.0 pIC50 = 10 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
11700433 77257 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 675 11 1 6 8.5 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)c2ccccc2)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL208812 77257 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 675 11 1 6 8.5 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)c2ccccc2)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
11707186 77877 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 1 7 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210709 77877 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 1 7 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
20691661 79203 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 79203 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
11512905 137890 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 137890 0 None - 0 Human 10.0 pIC50 = 10 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
155524081 170314 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)O[C@@H]1[C@@H](CO)O[C@@H](n2ccc(N)nc2=O)C1(F)F)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4454362 170314 0 None - 0 Human 10.0 pIC50 = 10.0 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)O[C@@H]1[C@@H](CO)O[C@@H](n2ccc(N)nc2=O)C1(F)F)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
10371708 63191 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 63191 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
44293177 174131 0 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45597 174131 0 None - 0 Rat 9.9 pIC50 = 9.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 13 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
67143119 175281 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4585638 175281 0 None - 0 Human 9.9 pIC50 = 9.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143780 171686 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4474379 171686 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
67143102 172363 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4516712 172363 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143023 174425 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4566719 174425 0 None - 0 Human 9.8 pIC50 = 9.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9895596 63185 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
CHEMBL1800152 63185 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.125I-Leuprorelin Binding Assay: The monkey and human membrane fractions prepared were diluted with the assay buffer to yield a 200 g/ml dilution, each of which was then dispensed at 188 μl per tube. To a tube containing the cell membrane fraction of the CHO with monkey GnRH receptors expressed were added 2 μl of a solution of 20 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To a tube containing the cell membrane fraction of the CHO with human GnRH receptors expressed were added 2 μl of a solution of 2 mM compound in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin. To determine maximum binding quantity, a reaction mixture containing 2 μl of 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared. To determine non-specific binding amount, a reaction mixture containing 2 μl of a solution of 100 μM leuprorelin in 60% DMSO and 10 μl of 38 nM 125I-leuprorelin was prepared.
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F nan
1184 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
9874838 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
CHEMBL71917 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
1184 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9875078 75576 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 680 11 1 8 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL20511 75576 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 680 11 1 8 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9853275 79431 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 681 11 2 8 6.9 CCONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21217 79431 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 681 11 2 8 6.9 CCONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9831689 98560 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 679 10 2 7 7.4 CC(C)NC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL280126 98560 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 679 10 2 7 7.4 CC(C)NC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
1184 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
9874838 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
CHEMBL71917 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
23656390 161134 0 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
CHEMBL413245 161134 0 None - 1 Rat 9.7 pIC50 = 9.7 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
44321964 95972 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL261979 95972 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
9895596 63185 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 63185 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386916 63187 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800154 63187 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 654 11 2 10 4.5 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(F)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386917 63189 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 63189 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53388959 63236 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccnc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800662 63236 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 668 10 2 9 5.9 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2cccnc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53389118 63241 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800667 63241 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 712 12 2 10 4.2 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCN(C)S(C)(=O)=O)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
53386756 63243 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800669 63243 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 617 13 2 10 3.6 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCOC)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386757 63244 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
CHEMBL1800670 63244 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 14 2 10 4.0 CCOCCn1c(=O)c2c(CN(C)CCOC)c(-c3ccc(NC(=O)NOC)cc3)sc2n(Cc2c(F)cccc2F)c1=O 10.1021/jm200216q
44293348 100026 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 100026 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293075 90233 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL239108 90233 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
18914263 96453 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL265774 96453 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44214108 100647 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295152 100647 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
21254068 101318 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300045 101318 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293070 165542 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL42592 165542 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
18914272 169114 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL443768 169114 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
21254089 181075 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47761 181075 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292988 181859 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47862 181859 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
18914248 187148 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL49542 187148 0 None - 0 Rat 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
1184 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
10794239 12953 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 1 7 7.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL1190107 12953 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 1 7 7.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL540109 12953 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 1 7 7.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
9809590 79227 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 6 8.1 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211503 79227 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 6 8.1 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
11643195 79419 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 2 7 7.2 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)(C)O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212121 79419 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 2 7 7.2 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)(C)O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11628915 137697 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 2 7 6.5 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CO)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL377015 137697 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 629 11 2 7 6.5 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CO)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11512905 137890 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 137890 0 None - 0 Human 9.7 pIC50 = 9.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
1184 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
9874838 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
CHEMBL71917 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
1184 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
9874838 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL71917 3676 31 None 426 2 Human 9.7 pIC50 = 9.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
118074127 175144 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4582367 175144 0 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44348308 81576 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL216519 81576 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
53387071 63190 4 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800157 63190 4 None - 0 Human 9.6 pIC50 = 9.6 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 12 2 12 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
44346805 168288 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1565 40 20 23 -2.2 CC(C)C[C@H](NC(=O)[C@H](CCCCNCc1cc(O)c2c(c1)C(=O)c1cc(C(=O)O)cc(O)c1C2=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
91931800 168288 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1565 40 20 23 -2.2 CC(C)C[C@H](NC(=O)[C@H](CCCCNCc1cc(O)c2c(c1)C(=O)c1cc(C(=O)O)cc(O)c1C2=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
CHEMBL438099 168288 0 None - 0 Rat 9.6 pIC50 = 9.6 Binding
Evaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptorsEvaluated for gonadotropin-releasing hormone receptor binding by displacing the 50% of the bound tracer [125I][D-Lys6]-GnRH radioligand in rat pituitary receptors
ChEMBL 1565 40 20 23 -2.2 CC(C)C[C@H](NC(=O)[C@H](CCCCNCc1cc(O)c2c(c1)C(=O)c1cc(C(=O)O)cc(O)c1C2=O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NOC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm010112g
1175 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
1559 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
657181 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
CHEMBL1201199 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
DB00007 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL None None None None 10.1039/C5MD00259A
145958346 161432 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 543 8 1 7 4.3 COc1ccc(F)cc1C(N)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4159155 161432 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 543 8 1 7 4.3 COc1ccc(F)cc1C(N)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1016/j.ejmech.2017.12.095
10100930 63188 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800155 63188 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 665 12 2 10 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)cc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10985312 78336 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 78336 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9896373 98592 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 1 8 7.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(NC(=O)C(C)C)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
CHEMBL280365 98592 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 1 8 7.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(NC(=O)C(C)C)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
44395623 124137 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL364167 124137 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 5.3 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10053165 183417 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL48192 183417 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44321052 204548 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86912 204548 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 578 9 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00512-1
44340906 9480 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112400 9480 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 578 9 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2)c1 10.1016/s0960-894x(02)00751-5
9985901 109964 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL324654 109964 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
1185 3645 32 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
53386758 63183 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 603 12 3 10 3.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCO)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800150 63183 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 603 12 3 10 3.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CCO)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386914 63184 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 12 3 10 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CC(C)(C)O)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800151 63184 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 631 12 3 10 3.8 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(CC(C)(C)O)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53389116 63239 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 672 11 2 11 4.6 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCn2ccnn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800665 63239 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 672 11 2 11 4.6 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)CCn2ccnn2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
9895596 63185 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800152 63185 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 636 11 2 10 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
53386915 63186 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800153 63186 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 650 11 2 10 4.7 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(C)cn1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
10009345 100452 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 642 11 2 8 5.8 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL293921 100452 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 642 11 2 8 5.8 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
44380643 58410 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
CHEMBL168498 58410 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 659 10 3 5 7.7 COC(=O)c1nc2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4ccc(C(C)(C)C(=O)N5CC6CCC5CC6)cc34)ccc2[nH]1 10.1016/s0960-894x(02)00026-4
44380625 58418 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168538 58418 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
10008768 58426 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168563 58426 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380488 58707 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169238 58707 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ocnc3c2)c1 10.1016/s0960-894x(02)00026-4
9894997 119808 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352806 119808 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44214098 100824 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296483 100824 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293443 183469 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48224 183469 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293148 186903 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49412 186903 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 524 12 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
9936150 188150 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50500 188150 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293054 101025 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297927 101025 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292977 173665 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45489 173665 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
1175 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
1559 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
657181 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
CHEMBL1201199 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
DB00007 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None None 10.1021/jm0512894
44348321 96081 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1520 39 15 17 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)c2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL262825 96081 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1520 39 15 17 2.3 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)c2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348306 156451 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407316 156451 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348399 160778 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL412472 160778 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348528 161378 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL415351 161378 0 None - 0 Rat 9.5 pIC50 = 9.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
10053165 183417 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/s0960-894x(00)00318-8
CHEMBL48192 183417 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/s0960-894x(00)00318-8
10053165 183417 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
CHEMBL48192 183417 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
9961721 167914 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 167914 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
1175 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
1559 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
657181 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
CHEMBL1201199 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
DB00007 2266 38 None - 1 Human 9.5 pIC50 = 9.5 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None None 10.1021/jm9803673
67144164 173314 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
CHEMBL4539811 173314 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
9961721 167914 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44395435 123295 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362371 123295 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 523 7 3 8 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
67143710 169768 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447139 169768 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10348973 3261 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3261 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3261 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3261 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3261 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counterDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
10348973 3261 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3261 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3261 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3261 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3261 50 None - 1 Rat 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
87285473 173518 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4544693 173518 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145955571 162109 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
CHEMBL4169891 162109 0 None - 0 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 721 13 2 9 5.2 Cc1cc(F)cc([C@H](Cn2c(=O)c(N3CCN(Cc4ccc(C(F)(F)F)o4)CC3)c(C)n(Cc3c(F)cccc3F)c2=O)NCCCC(=O)O)c1 10.1016/j.ejmech.2017.12.095
10348973 3261 50 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5432 3261 50 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
5586 3261 50 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
CHEMBL1800159 3261 50 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
DB11853 3261 50 None - 1 Human 9.5 pIC50 = 9.5 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/jm200216q
67144353 171657 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4474058 171657 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145954246 161858 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 529 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4165983 161858 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 529 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44348533 161191 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL413752 161191 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)cc1 10.1021/jm970024p
67143773 169937 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449450 169937 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143621 170737 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4460880 170737 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
87285554 172758 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526641 172758 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9917618 98189 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 653 9 3 8 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NO)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
CHEMBL277214 98189 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 653 9 3 8 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NO)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
10919567 98573 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL280213 98573 0 None - 1 Human 9.4 pIC50 = 9.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44321963 105461 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
CHEMBL312864 105461 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 6.8 COCn1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccc1=O 10.1016/s0960-894x(01)00512-1
44321411 106526 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315326 106526 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@@H]5CC[C@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321345 204519 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86758 204519 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 596 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCC2CCC(=O)N(C)C2)c1 10.1016/s0960-894x(01)00512-1
44293163 188115 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL50433 188115 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44341082 9685 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113574 9685 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 9 2 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)nc(C)c2)c1 10.1016/s0960-894x(02)00751-5
44341046 9981 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL115365 9981 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 634 11 2 5 7.5 CC(=O)OCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
44340888 110036 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL325091 110036 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 10 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(CO)c2)c1 10.1016/s0960-894x(02)00751-5
1185 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
9895731 201746 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 644 11 2 9 5.4 CONC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL65769 201746 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 644 11 2 9 5.4 CONC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
9873212 57272 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166649 57272 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
9938925 57287 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166763 57287 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 616 11 3 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2c[nH]c3ncnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44380626 58419 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168539 58419 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380537 96113 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL263004 96113 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
44380394 119443 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL349638 119443 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380514 119707 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352051 119707 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 645 10 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(=O)O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
9809394 120004 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL354524 120004 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 628 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44292940 100794 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296244 100794 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293651 162564 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417726 162564 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 10 2 4 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293335 172058 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 172058 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293349 183542 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48273 183542 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 16 2 3 8.0 CCCCN(CCCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
10258643 100913 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297151 100913 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 644 16 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293178 100952 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297430 100952 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293074 187200 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49578 187200 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
11614283 77771 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 627 11 1 6 7.9 CCC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210321 77771 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 627 11 1 6 7.9 CCC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11592777 138723 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 2 6 8.0 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL378979 138723 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 643 11 2 6 8.0 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
44413067 138770 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 593 11 1 7 6.9 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL379198 138770 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 593 11 1 7 6.9 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44352512 116796 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
CHEMBL339636 116796 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
67143509 169498 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4443108 169498 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44348324 156736 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407681 156736 0 None - 0 Rat 9.4 pIC50 = 9.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44309572 202636 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
CHEMBL71561 202636 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
10649568 14397 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL120432 14397 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/j.bmcl.2004.08.056
87285768 169927 1 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169927 1 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10649568 14397 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of binding to GnRH receptor in humanIn vitro inhibition of binding to GnRH receptor in human
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14397 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
In vitro inhibition of binding to GnRH receptor in humanIn vitro inhibition of binding to GnRH receptor in human
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
10649568 14397 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
CHEMBL120432 14397 0 None 10 2 Human 9.4 pIC50 = 9.4 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
67142732 169056 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436854 169056 0 None - 0 Human 9.4 pIC50 = 9.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145949496 162308 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL4173065 162308 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 685 13 2 9 4.9 Cc1cccc(F)c1Cn1c(C)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.ejmech.2017.12.095
CHEMBL2370593 208131 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](N)C(N)=O)cc1 10.1021/jm970024p
44460342 167359 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL431402 167359 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 9 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)[n+]([O-])c(C)c2)c1 10.1016/s0960-894x(02)00751-5
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
18324807 63242 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800668 63242 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 635 11 2 9 5.0 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
1185 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 9.3 pIC50 = 9.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
10649568 14397 0 None 10 2 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkeyIn vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkey
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14397 0 None 10 2 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkeyIn vitro inhibition of gonadotropin-releasing hormone receptor in rhesus monkey
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
9809382 100208 0 None - 1 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL292291 100208 0 None - 1 Human 9.3 pIC50 = 9.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
44380538 58776 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169620 58776 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 619 9 2 5 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3nsnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293591 101125 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 101125 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293129 181154 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47772 181154 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 510 11 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293213 187218 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49590 187218 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293071 101130 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL298748 101130 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293366 161662 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL416285 161662 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
1175 2266 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
1559 2266 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
657181 2266 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
CHEMBL1201199 2266 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
DB00007 2266 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
CHEMBL2370590 208129 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CCNC(C)C)cc1 10.1021/jm970024p
44293205 183379 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 643 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)ccc1I 10.1016/s0960-894x(00)00318-8
CHEMBL48165 183379 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 643 7 3 7 6.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)ccc1I 10.1016/s0960-894x(00)00318-8
44295699 100751 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL295948 100751 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
9828888 101355 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL300295 101355 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
1175 2266 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
1559 2266 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
657181 2266 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
CHEMBL1201199 2266 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
DB00007 2266 38 None - 1 Rat 9.3 pIC50 = 9.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None None 10.1021/jm9803673
44348325 96161 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](NC(=O)c2ccc(NC(C)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL263358 96161 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@@H](NC(=O)[C@@H](NC(=O)c2ccc(NC(C)=O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL2370592 208130 0 None - 0 Rat 9.3 pIC50 = 9.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CC(C)C)cc1 10.1021/jm970024p
44395462 167660 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL433594 167660 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 551 7 3 8 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10371708 63191 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
CHEMBL1800158 63191 0 None - 0 Human 9.3 pIC50 = 9.3 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 622 9 2 10 4.4 CONC(=O)Nc1ccc(-c2sc3c(c2CN(C)C)c(=O)n(-c2ccc(OC)nc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm200216q
155531714 175617 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175617 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
58239302 161441 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4159247 161441 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 12 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(C)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11167850 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1178 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1187 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL179691 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
11167850 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
1178 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
1187 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
CHEMBL179691 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.ejmech.2017.12.095
44348454 156678 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407615 156678 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
1184 3676 31 None -426 2 Rat 9.2 pIC50 = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
9874838 3676 31 None -426 2 Rat 9.2 pIC50 = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
CHEMBL71917 3676 31 None -426 2 Rat 9.2 pIC50 = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(02)00370-0
9896737 82954 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 695 11 2 8 7.3 CC(C)ONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21936 82954 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 695 11 2 8 7.3 CC(C)ONC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9893269 65964 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL184819 65964 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 532 7 2 7 6.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10187208 66415 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185785 66415 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 540 7 2 9 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2OCCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44395533 66465 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185986 66465 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 577 7 2 8 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CC3CCN2CC3)cc(C)c1C 10.1016/j.bmcl.2004.08.056
10231401 1989 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
5584 1989 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
CHEMBL314260 1989 1 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1016/s0960-894x(01)00512-1
44321148 96360 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265042 96360 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 622 11 2 5 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CC4)OCCO5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44320895 163710 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL421160 163710 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccnc2)c1 10.1016/s0960-894x(01)00512-1
44321393 204547 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86911 204547 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 606 9 2 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc(C)c(=O)n(C)c2)c1 10.1016/s0960-894x(01)00512-1
44340928 9652 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL113432 9652 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
44340929 113003 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL332049 113003 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 10 2 4 7.7 CC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
67143618 169727 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446435 169727 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9960399 50271 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL157412 50271 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 603 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2c[nH]c3nnnc-3c2)c1 10.1016/s0960-894x(02)00026-4
44380512 57132 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165456 57132 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380236 58413 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168506 58413 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 641 11 2 4 8.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
44380796 58891 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170159 58891 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 598 9 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
44380798 59014 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170606 59014 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 588 9 3 4 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]nnc3c2)c1 10.1016/s0960-894x(02)00026-4
44380536 119885 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353395 119885 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 602 9 2 4 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3ncoc3c2)c1 10.1016/s0960-894x(02)00026-4
44293273 161543 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL416102 161543 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44293592 162340 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 162340 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44292918 170849 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 170849 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293134 186818 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 186818 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293411 188182 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50552 188182 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 494 10 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44412890 77907 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 607 11 1 7 7.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210888 77907 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 607 11 1 7 7.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44295753 186164 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
CHEMBL48879 186164 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.5 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to LHRH receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm020180i
44348453 96672 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
CHEMBL267642 96672 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 42 15 17 2.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](NC=O)C(N)=O)cc1 10.1021/jm970024p
44348316 96083 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL262842 96083 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348148 156209 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407058 156209 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348527 161284 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL414558 161284 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 14 16 3.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL2370594 208132 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C(N)=O)N(C)C=O)cc1 10.1021/jm970024p
87285708 173333 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4540232 173333 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
155517188 169596 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4444427 169596 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1542 39 20 23 -4.2 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
44395502 165345 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL424991 165345 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 553 7 3 9 5.0 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2COCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
9808288 110993 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL327704 110993 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321498 204582 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87099 204582 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44341197 108548 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL321258 108548 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 587 9 2 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C#N)c2)c1 10.1016/s0960-894x(02)00751-5
44341198 112559 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL331144 112559 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(C)(C)O)c2)c1 10.1016/s0960-894x(02)00751-5
44460343 203634 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL79639 203634 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 11 2 4 7.6 COCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
11167850 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 9.2 pIC50 = 9.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44305285 100151 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 630 11 2 9 5.0 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NOC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL291896 100151 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 630 11 2 9 5.0 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NOC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
44380478 58447 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168637 58447 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
44380483 58766 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169569 58766 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 635 9 4 4 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2F)c1 10.1016/s0960-894x(02)00026-4
9808288 110993 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL327704 110993 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 576 11 2 3 8.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(02)00026-4
44380513 119686 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL351836 119686 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 631 10 4 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(CO)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44292919 100676 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 100676 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293650 161779 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL416470 161779 0 None - 0 Rat 9.2 pIC50 = 9.2 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293045 185242 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 7 5.7 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc4c(c3)CCC4)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48674 185242 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 7 5.7 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc4c(c3)CCC4)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
44293206 186606 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1ccc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
CHEMBL49230 186606 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1ccc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)cc1C 10.1016/s0960-894x(00)00318-8
145955844 162142 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 7 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(C)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4170478 162142 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 7 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(C)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44348534 161277 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 37 16 17 -0.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)NC(NC(=O)CN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
91935482 161277 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 37 16 17 -0.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)NC(NC(=O)CN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL414469 161277 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 37 16 17 -0.4 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)NC(NC(=O)CN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348307 161276 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL414468 161276 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44395491 123332 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL362544 123332 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 531 7 3 7 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCN2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44321412 204529 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86805 204529 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321290 204680 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87785 204680 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44341164 9473 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL112378 9473 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 592 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cc[n+]([O-])cc2C)c1 10.1016/s0960-894x(02)00751-5
44341056 114036 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
CHEMBL333614 114036 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccncc2C)c1 10.1016/s0960-894x(02)00751-5
1185 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
1185 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL None None None None 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
53386917 63189 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
CHEMBL1800156 63189 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 666 12 2 11 4.4 COCCN(C)Cc1c(-c2ccc(NC(=O)NOC)cc2)sc2c1c(=O)n(-c1ccc(OC)nc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm200216q
71449058 83985 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111955 83985 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2219718 83985 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44380222 57291 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166778 57291 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 614 10 2 5 7.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cnc3nccnc3c2)c1 10.1016/s0960-894x(02)00026-4
44293605 100704 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295591 100704 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 468 10 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44292874 183258 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48069 183258 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 616 13 3 4 7.2 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)(C)C 10.1016/s0960-894x(01)00274-8
1175 2266 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
1559 2266 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
657181 2266 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
CHEMBL1201199 2266 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
DB00007 2266 38 None - 1 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None None 10.1021/jm0512894
1175 2266 38 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
1559 2266 38 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
657181 2266 38 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
CHEMBL1201199 2266 38 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
DB00007 2266 38 None - 1 Rat 9.1 pIC50 = 9.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None None 10.1021/jm9803673
44348056 159471 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL410798 159471 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1545 41 14 16 3.1 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348400 168128 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL436683 168128 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44395583 123827 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL363663 123827 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 524 7 2 8 5.8 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCO2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44341113 9828 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL114438 9828 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 576 9 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C)c2)c1 10.1016/s0960-894x(02)00751-5
44341199 112560 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL331145 112560 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 620 10 2 5 7.2 COC(=O)c1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
9961721 167914 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
11167850 2701 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.1 pIC50 = 9.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44295755 192519 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL2111956 192519 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL52278 192519 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44380681 58466 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168726 58466 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 669 9 3 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(C(F)(F)F)nc3c2)c1 10.1016/s0960-894x(02)00026-4
44380147 119772 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352566 119772 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
20691661 79203 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 79203 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
44348057 96010 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL262309 96010 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL2370589 208128 0 None - 0 Rat 9.1 pIC50 = 9.1 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL None None None CN[C@@H](NC(=O)[C@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(C)=O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(N)=O 10.1021/jm970024p
44293222 175387 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL138464 175387 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL45883 175387 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44295755 192519 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL2111956 192519 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL52278 192519 0 None - 0 Human 9.1 pIC50 = 9.1 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
67143518 174302 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4563562 174302 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
87285476 170901 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4463476 170901 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11017929 98564 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 624 9 1 8 6.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(N)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
CHEMBL280170 98564 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 624 9 1 8 6.4 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc(N)cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
10930638 98572 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
CHEMBL280212 98572 0 None - 0 Human 9.0 pIC50 = 9 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm020180i
44321101 96400 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL265288 96400 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321394 106456 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
CHEMBL314860 106456 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 10 2 4 7.5 COc1ccc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)cn1 10.1016/s0960-894x(01)00512-1
44321410 106525 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315325 106525 0 None - 0 Human 9.0 pIC50 = 9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 576 11 2 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11167850 2701 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
87285565 169702 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446131 169702 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143755 174853 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4576169 174853 0 None - 0 Human 9.0 pIC50 = 9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9961721 167914 0 None - 1 Human 9.0 pIC50 = 9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 9.0 pIC50 = 9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44293377 101433 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL300865 101433 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 12 2 3 7.8 CCC(C)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293347 162561 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL417720 162561 0 None - 0 Rat 9.0 pIC50 = 9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC(C)(C)C4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44412945 96258 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 7 7.8 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL264121 96258 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 641 11 1 7 7.8 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44293386 174959 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL45784 174959 0 None - 0 Human 9.0 pIC50 = 9 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)c(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
67143613 170459 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456703 170459 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
22129998 100805 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL296321 100805 0 None - 0 Rat 9.0 pIC50 = 9.0 Binding
Compound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptorCompound was evaluated for its inhibitory activity against rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
11167850 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL None None None None 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3645 32 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
87285570 170175 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4452347 170175 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143804 172625 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4522657 172625 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285767 174305 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4563686 174305 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9961721 167914 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 9.0 pIC50 = 9.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44380146 119771 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352565 119771 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 627 10 2 4 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccnc3nc(C)ccc23)c1 10.1016/s0960-894x(02)00026-4
44380318 119873 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL353308 119873 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
44380487 167018 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL430069 167018 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 601 9 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]ncc3c2)c1 10.1016/s0960-894x(02)00026-4
44292950 161895 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL416651 161895 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44292868 176333 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL46177 176333 0 None - 0 Human 9.0 pIC50 = 9.0 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 571 7 3 7 6.5 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3cc(Cl)cc(Cl)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
67143547 170950 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464132 170950 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44320921 106685 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316362 106685 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 548 9 2 3 7.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CC[C@@H]4C5)cc3c2[C@H](C)CNCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67143761 170795 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4461692 170795 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285550 173756 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4550720 173756 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44293555 100740 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295897 100740 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 574 11 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C4(C(=O)N5C6CCC5CC6)CCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44348297 166906 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL429902 166906 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
145953172 161922 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(Cl)cc(Cl)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4167067 161922 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cc(Cl)cc(Cl)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL415547 211441 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
67143505 171664 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 601 8 1 8 4.6 Cc1c(N2CCN(Cc3cccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4474116 171664 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 601 8 1 8 4.6 Cc1c(N2CCN(Cc3cccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44321146 105924 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313946 105924 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC(C)(C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 209243 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3645 32 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3645 32 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3645 32 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3645 32 None - 1 Rat 8.9 pIC50 = 8.9 Binding
Displacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from rat GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL415547 211441 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@H](Cc1ccc(Nc2n[nH]c(N)n2)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44395677 66405 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185738 66405 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 565 7 2 8 5.7 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCC[C@H]2CCC(=O)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44293249 184861 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL48616 184861 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321509 204468 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86431 204468 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C[C@H]5CCCC[C@H]5C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44359285 11522 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180695 11522 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138747 11522 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 7 3 7 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(Cl)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293249 184861 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48616 184861 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44215053 185038 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL48641 185038 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 562 11 2 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44348149 168153 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL436897 168153 0 None - 0 Rat 8.9 pIC50 = 8.9 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
67143570 171191 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467407 171191 0 None - 0 Human 8.9 pIC50 = 8.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
23656390 161134 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
CHEMBL413245 161134 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1021/jm701249f
11167850 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL None None None None 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67142962 174004 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 629 9 1 8 4.6 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4556717 174004 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 629 9 1 8 4.6 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44380797 58980 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL170499 58980 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3cnccc23)c1 10.1016/s0960-894x(02)00026-4
44215055 100820 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL296442 100820 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 576 11 1 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(C)CCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44593425 176191 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
CHEMBL460480 176191 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
11167850 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
3038517 3645 32 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
CHEMBL22055 3645 32 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
DB06494 3645 32 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serumDisplacement of [125I]leuprorelin from recombinant human GnRH receptor expressed in CHO cells after 60 mins by X-ray counter in presence of 40% fetal bovine serum
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm200216q
70689073 77273 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
91900370 77273 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2088253 77273 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
155531714 175617 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175617 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
10231401 1989 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity at rat GnRH receptor by whole cell binding assayBinding affinity at rat GnRH receptor by whole cell binding assay
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1021/jm701249f
5584 1989 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity at rat GnRH receptor by whole cell binding assayBinding affinity at rat GnRH receptor by whole cell binding assay
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1021/jm701249f
CHEMBL314260 1989 1 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Binding affinity at rat GnRH receptor by whole cell binding assayBinding affinity at rat GnRH receptor by whole cell binding assay
ChEMBL 562 9 2 3 7.5 Cc1cc(C)cc(c1)c1[nH]c2c(c1[C@@H](CNCCc1ccncc1)C)cc(cc2)C(C(=O)N1CC2CCC1CC2)(C)C 10.1021/jm701249f
44593425 176191 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
CHEMBL460480 176191 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
44593425 176191 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 176191 0 None - 1 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
11167850 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
67144370 174043 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4557575 174043 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44293488 101084 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL298366 101084 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293376 101205 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299301 101205 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 13 2 3 8.2 CCC(CC)(C(=O)N1C2CCC1CC2)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44348172 155211 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1547 39 14 17 1.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(C)=O)cc1 10.1021/jm970024p
CHEMBL405736 155211 0 None - 0 Rat 8.8 pIC50 = 8.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1547 39 14 17 1.8 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(C)=O)cc1 10.1021/jm970024p
44402640 161281 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
CHEMBL414514 161281 0 None - 0 Human 8.8 pIC50 = 8.8 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
11167850 2701 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
87285770 175470 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
CHEMBL4590493 175470 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
11620431 178789 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 178789 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44359264 11523 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180700 11523 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138866 11523 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293802 101562 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL301802 101562 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 550 11 2 3 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293081 182122 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL47895 182122 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44402639 154690 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL402671 154690 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
164628446 185730 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assayDisplacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assay
ChEMBL 1627 43 20 26 -5.2 CC(C)CC(NC(=O)C(CCCCNC(=O)/C=N/OCC(=O)OCC1OC(n2ccc(N)nc2=O)C(F)(F)C1O)NC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CO)NC(=O)C(Cc1cc2ccccc2[nH]1)NC(=O)C(Cc1c[nH]cn1)NC(=O)C1CCC(=O)N1)C(=O)NC(CCCNC(=N)N)C(=O)N1CCCC1C(=O)NCC(N)=O 10.1016/j.ejmech.2020.113018
CHEMBL4874610 185730 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assayDisplacement of [125I]-DTrp6-LHRH from human GnRH-R by radioligand binding assay
ChEMBL 1627 43 20 26 -5.2 CC(C)CC(NC(=O)C(CCCCNC(=O)/C=N/OCC(=O)OCC1OC(n2ccc(N)nc2=O)C(F)(F)C1O)NC(=O)C(Cc1ccc(O)cc1)NC(=O)C(CO)NC(=O)C(Cc1cc2ccccc2[nH]1)NC(=O)C(Cc1c[nH]cn1)NC(=O)C1CCC(=O)N1)C(=O)NC(CCCNC(=N)N)C(=O)N1CCCC1C(=O)NCC(N)=O 10.1016/j.ejmech.2020.113018
CHEMBL436874 211941 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL None None None None 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
10438167 100712 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL295641 100712 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 578 12 2 3 8.6 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCCCC1 10.1016/s0960-894x(01)00275-x
44380319 58442 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168615 58442 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44348174 159497 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
CHEMBL410818 159497 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
67143612 170483 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456937 170483 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402639 154690 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL402671 154690 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1603 41 16 17 2.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)[C@@H]2CCC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402518 157980 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL409138 157980 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402640 161281 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
CHEMBL414514 161281 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1617 41 17 17 2.0 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C2CCNC(=O)N2)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
91810333 178998 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
CHEMBL4741994 178998 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
118179218 179435 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4747248 179435 0 None - 0 Human 8.0 pIC50 = 8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
10004181 100617 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL294910 100617 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
44573110 186611 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL492327 186611 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44573113 192635 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL523711 192635 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
1185 3645 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44577104 178169 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 178169 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
67143054 169721 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 581 8 1 7 3.9 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4446360 169721 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 581 8 1 7 3.9 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
53239181 171937 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4483419 171937 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1185 3645 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 8.0 pIC50 = 8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44305605 201640 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 613 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL64920 201640 0 None - 0 Human 8.0 pIC50 = 8 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 613 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11214294 121681 0 None 912 2 Human 8.0 pIC50 = 8 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 121681 0 None 912 2 Human 8.0 pIC50 = 8 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL438652 212037 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm0512894
44293111 100748 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL295917 100748 0 None - 0 Human 8.0 pIC50 = 8 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
10004181 100617 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL294910 100617 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
15895698 205152 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL90725 205152 0 None - 0 Rat 8.0 pIC50 = 8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/j.bmcl.2003.12.101
11980076 206711 27 None - 1 Human 8.0 pIC50 = 8 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL1007 206711 27 None - 1 Human 8.0 pIC50 = 8 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL436874 211941 0 None - 0 Human 8.0 pIC50 = 8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL None None None None 10.1021/jm0506928
CHEMBL448249 212205 13 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL436874 211941 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL None None None None 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44359456 12098 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184286 12098 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342908 12098 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 572 8 3 6 7.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccc(N(C)C)cc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44322384 105659 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL313501 105659 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
44365638 41680 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 518 12 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(OCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL149441 41680 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 518 12 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(OCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44214104 121242 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 540 10 4 5 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCNCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL358901 121242 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 540 10 4 5 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCNCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44444617 93711 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249372 93711 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
10930638 98572 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322165 204495 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 458 5 1 4 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(C(F)(F)F)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL86609 204495 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 458 5 1 4 6.5 Cc1cc(C)cc(-c2c(O)nc3cc(C(F)(F)F)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
11599857 76525 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 597 11 0 9 6.5 CCOC(=O)c1cn(Cc2ccccc2[N+](=O)[O-])c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL206964 76525 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 597 11 0 9 6.5 CCOC(=O)c1cn(Cc2ccccc2[N+](=O)[O-])c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11520078 79315 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 577 10 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2C#N)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211588 79315 0 None - 0 Human 7.0 pIC50 = 7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 577 10 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2C#N)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44365131 38287 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 472 13 3 4 6.5 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL146451 38287 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 472 13 3 4 6.5 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44364998 40212 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 443 11 3 4 5.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL148246 40212 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 443 11 3 4 5.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
10808668 204894 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 362 4 1 4 5.2 Oc1nc2cc(Cl)ccc2c(OCc2ccccn2)c1-c1ccccc1 10.1016/s0960-894x(99)00446-1
CHEMBL89086 204894 0 None - 0 Rat 5.0 pIC50 = 5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 362 4 1 4 5.2 Oc1nc2cc(Cl)ccc2c(OCc2ccccn2)c1-c1ccccc1 10.1016/s0960-894x(99)00446-1
10837806 77672 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 463 7 0 7 5.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(C)c2c1=O 10.1021/jm0512894
CHEMBL209836 77672 0 None - 0 Human 5.0 pIC50 = 5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 463 7 0 7 5.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(C)c2c1=O 10.1021/jm0512894
162653870 179961 0 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4753775 179961 0 None - 0 Human 5.0 pIC50 = 5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
44406776 133819 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.0 pIC50 = 7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44444642 93934 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250770 93934 0 None - 0 Rat 7.0 pIC50 = 7 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67142732 169056 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436854 169056 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 640 9 1 9 4.5 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44417615 141391 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
67143815 170974 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464440 170974 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143102 172363 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4516712 172363 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 9 4.0 Cc1c(N2CCN(Cc3ccc(C#N)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
71623059 180243 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 180243 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44444645 154461 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL401351 154461 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
162673323 182534 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4794864 182534 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
86274853 115687 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
CHEMBL3358414 115687 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
1185 3645 32 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
67143030 172546 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(F)c3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4520639 172546 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(F)c3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44444668 153745 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL398648 153745 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143633 172738 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526188 172738 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL2370265 208080 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](Cc1ccccn1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm990433g
44573275 186832 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493730 186832 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
44406776 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44293151 100705 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
CHEMBL295595 100705 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 2 3 6.9 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C(C)C 10.1016/s0960-894x(01)00275-x
44293250 101263 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299615 101263 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 552 11 2 4 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44406776 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
145973124 162472 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 595 8 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(C(F)(F)F)cc3F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4175801 162472 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 595 8 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(C(F)(F)F)cc3F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11167850 2701 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL409218 211006 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N1CCC[C@@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11496945 175901 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 175901 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
21899433 154164 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399772 154164 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44346397 114000 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
1185 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44359193 11533 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180764 11533 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141750 11533 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)NCc4ccc5c(c4)OCO5)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44402335 71272 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196337 71272 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402468 132299 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370144 132299 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
70697569 77620 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL2096778 77620 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
11720984 63149 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL179885 63149 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
162645007 178881 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44346398 14369 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14369 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 141086 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113244 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
15462666 96055 4 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96055 4 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391541 65260 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183237 65260 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391525 165813 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL427500 165813 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365375 121002 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 9 3 2 5.8 Oc1ccc(CCCCNCCc2c(-c3ccc(F)cc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL358416 121002 0 None - 0 Rat 5.0 pIC50 = 5.0 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 9 3 2 5.8 Oc1ccc(CCCCNCCc2c(-c3ccc(F)cc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
11619758 172643 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 470 6 3 5 5.0 S=c1[nH]c2cccc(OCCN3CCN(c4cccc5[nH]c(-c6ccccc6)nc45)CC3)c2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL452293 172643 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 470 6 3 5 5.0 S=c1[nH]c2cccc(OCCN3CCN(c4cccc5[nH]c(-c6ccccc6)nc45)CC3)c2[nH]1 10.1016/j.bmc.2008.05.024
162645007 178881 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
67144335 169271 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 658 9 1 9 4.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4439926 169271 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 658 9 1 9 4.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 3645 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
118179127 182632 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
CHEMBL4795998 182632 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
44444676 154399 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401080 154399 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444641 154430 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401212 154430 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143413 169050 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4436711 169050 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
44365877 118975 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 13 3 6 6.2 CCCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL345297 118975 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 13 3 6 6.2 CCCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44573789 186757 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493167 186757 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
11496610 4012 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 4012 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 4012 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
11532637 7633 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 7633 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
53238728 170107 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 545 8 1 7 3.7 Cc1c(N2CCN(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4451627 170107 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 545 8 1 7 3.7 Cc1c(N2CCN(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
11496610 4012 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 4012 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 4012 11 None - 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
1185 3645 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44391752 161113 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL413062 161113 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
1185 3645 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL None None None None 10.1021/jm0506928
87285476 170901 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4463476 170901 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 8 1 8 5.2 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL436874 211941 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL None None None None 10.1021/jm0506928
44573278 186864 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL493932 186864 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44573628 192614 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
CHEMBL523527 192614 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
25194091 188423 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL508898 188423 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
25193797 189073 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL515200 189073 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
1185 3645 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 6.9 pIC50 = 6.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44267232 9526 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 454 10 3 3 6.0 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
CHEMBL11263 9526 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 454 10 3 3 6.0 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
44402647 69486 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL193740 69486 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
11525693 69487 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL193749 69487 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
11237922 65189 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
11237922 65189 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183066 65189 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183066 65189 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
25194092 189284 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 6 3 5 5.6 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)c(C)c1 10.1016/j.bmc.2008.05.024
CHEMBL516934 189284 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 6 3 5 5.6 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)c(C)c1 10.1016/j.bmc.2008.05.024
44417614 141086 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391541 65260 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183237 65260 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 482 9 1 7 4.6 CCSc1nc2cc(S(=O)(=O)NCc3ccc([N+](=O)[O-])cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
87285767 174305 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4563686 174305 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 2 10 5.1 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCS(=O)(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11167850 2701 22 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44267270 10280 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 450 9 2 1 7.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc3c(c2)CCCC3)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11623 10280 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 450 9 2 1 7.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc3c(c2)CCCC3)c1 10.1016/s0960-894x(01)00133-0
162652474 179869 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4752711 179869 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
67144367 169295 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 454 6 1 6 3.3 Cc1c(N2CCCCC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4440296 169295 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 454 6 1 6 3.3 Cc1c(N2CCCCC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
87285768 169927 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169927 1 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162650892 179649 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 179649 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
10930638 98572 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44406776 133819 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
67144085 170604 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccccc3[N+](=O)[O-])CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4458877 170604 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccccc3[N+](=O)[O-])CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44406776 133819 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67144307 172458 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 546 8 1 8 3.1 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4518726 172458 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 546 8 1 8 3.1 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44365486 38882 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3cccc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL146921 38882 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3cccc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL329807 209574 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL408737 210981 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44402467 170089 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL445143 170089 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
44402647 69486 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL193740 69486 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 604 11 3 8 6.5 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
44365119 119145 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 9 3 2 5.7 Oc1ccc(CCCCNCCc2c(-c3ccccc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL346852 119145 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 9 3 2 5.7 Oc1ccc(CCCCNCCc2c(-c3ccccc3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
25194090 188341 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL507973 188341 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 484 6 3 5 5.3 Cc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44346398 14369 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14369 0 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322240 204685 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 3 1 4 5.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL87804 204685 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 3 1 4 5.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
44322436 204938 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 4 1 4 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89387 204938 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 4 1 4 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
123549935 178854 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4740379 178854 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
162647697 179279 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4745391 179279 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44444665 93767 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249772 93767 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL2430899 208715 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
118179265 179931 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 619 5 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4753358 179931 0 None - 0 Human 4.9 pIC50 = 4.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 619 5 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(C(F)(F)F)cc1)C2C 10.1021/acs.jmedchem.0c01076
118178983 182849 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4798682 182849 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
44406776 133819 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44328452 96002 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1072 26 9 12 1.9 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCNNC(=O)c1cccnc1)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL262190 96002 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1072 26 9 12 1.9 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCNNC(=O)c1cccnc1)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
53238731 170409 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccc(Cl)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4456075 170409 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccc(Cl)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44214070 178594 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 561 13 3 5 6.2 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL47227 178594 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 561 13 3 5 6.2 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44391808 65264 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183274 65264 0 None - 0 Rat 7.9 pIC50 = 7.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67144408 175336 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3ccon3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4587044 175336 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3ccon3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67144409 170539 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
CHEMBL4457786 170539 0 None - 0 Human 7.9 pIC50 = 7.9 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144509 173557 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 575 9 1 8 3.7 COc1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4546034 173557 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 575 9 1 8 3.7 COc1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
162672599 182425 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4793643 182425 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
44328414 96008 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1028 23 9 10 2.2 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)Nc1ccccc1C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL262292 96008 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 1028 23 9 10 2.2 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)Nc1ccccc1C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44402404 133041 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL371073 133041 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
11237922 65189 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
11237922 65189 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183066 65189 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183066 65189 0 None - 0 Rat 6.9 pIC50 = 6.9 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1cccnc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
15462666 96055 4 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96055 4 None - 1 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 141086 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417615 141391 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322077 204817 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 421 5 1 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc([N+](=O)[O-])ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL88620 204817 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 421 5 1 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc([N+](=O)[O-])ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
44322441 205081 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 412 4 1 5 4.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CN(C)CCO2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL90383 205081 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 412 4 1 5 4.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CN(C)CCO2)c1 10.1016/s0960-894x(99)00446-1
44391574 65759 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
CHEMBL183847 65759 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
162667361 181943 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
CHEMBL4787218 181943 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
162645007 178881 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44322399 204556 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 7 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCCC2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL86955 204556 0 None - 0 Rat 5.9 pIC50 = 5.9 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 7 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCCC2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
71666542 179767 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4751345 179767 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
67143761 170795 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4461692 170795 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 710 12 3 9 3.8 Cc1c(N2CCN(Cc3cccc(C(=O)NCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 3645 32 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
118179051 179638 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179638 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
44322440 111071 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL328063 111071 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 6 2 6 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCN2)c1 10.1016/s0960-894x(99)00447-3
44365626 205215 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 596 11 3 5 6.4 CCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL91146 205215 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 596 11 3 5 6.4 CCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL436874 211941 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL None None None None 10.1021/jm0506928
9918188 154183 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399856 154183 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
10930638 98572 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44359252 11526 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180715 11526 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139291 11526 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 7 6.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccnc(C5CC5)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
71461676 79089 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL2113717 79089 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCC[C@H](C)N2)c1 10.1016/j.bmcl.2003.12.101
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44380192 57146 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 57146 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
70691931 73840 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023088 73840 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
15895698 205152 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL90725 205152 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 455 6 2 6 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2)c1 10.1016/s0960-894x(99)00447-3
44322166 204542 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 468 5 1 4 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Br)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL86897 204542 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 468 5 1 4 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Br)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
20691661 79203 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211485 79203 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 12 2 7 7.2 CCC(O)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
9909560 9781 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11420 9781 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44402492 125663 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
CHEMBL364933 125663 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
44391718 65274 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183325 65274 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44365093 118756 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 520 9 3 2 7.7 Oc1ccc(CCCCNCCc2c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL343658 118756 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 520 9 3 2 7.7 Oc1ccc(CCCCNCCc2c(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
162645007 178881 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL264526 208880 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44560995 178574 0 None - 3 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 178574 0 None - 3 Human 5.8 pIC50 = 5.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
10919052 113020 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113020 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10930638 98572 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402232 71067 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195920 71067 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402072 71395 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196616 71395 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44561265 172538 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL452044 172538 0 None - 0 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44560995 178574 0 None - 3 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL472117 178574 0 None - 3 Rat 4.8 pIC50 = 4.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 5 2 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
67143374 171175 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467261 171175 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162645007 178881 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
162675445 182826 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4798298 182826 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
44444647 154462 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401352 154462 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
71668147 179410 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4746969 179410 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
86275342 115686 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL3358413 115686 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44365793 120864 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 11 4 4 6.4 CCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL358126 120864 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 11 4 4 6.4 CCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL97540 214149 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44444635 154166 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399779 154166 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
145957339 161759 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3c(F)cccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4164508 161759 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3c(F)cccc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44572286 180219 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 180219 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
10046374 9067 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL11009 9067 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
10046374 9067 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11009 9067 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143780 171686 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4474379 171686 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 9 1 8 4.7 CC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL436874 211941 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL None None None None 10.1021/jm0506928
44380624 58826 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL169873 58826 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 587 8 3 3 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCc2ccc3[nH]cnc3c2)c1 10.1016/s0960-894x(02)00026-4
56655880 73839 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023087 73839 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
70689073 77273 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
91900370 77273 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2088253 77273 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1835 43 23 28 -2.7 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL436874 211941 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL None None None None 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44346667 113244 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 6.8 pIC50 = 6.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44267237 97921 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL275287 97921 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44402560 71092 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 1 5 5.9 COc1ccc(Cl)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196088 71092 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 1 5 5.9 COc1ccc(Cl)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402468 132299 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370144 132299 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
44402256 135756 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL373340 135756 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
11330164 64872 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182513 64872 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44346398 14369 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14369 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113244 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10919052 113020 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113020 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
15462666 96055 4 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96055 4 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402426 132236 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL370028 132236 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391849 122439 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360743 122439 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
162673323 182534 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4794864 182534 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccccc4Cl)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
21899433 154164 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399772 154164 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 631 8 1 6 5.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44406776 133819 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143135 173950 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4555444 173950 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444670 94043 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251388 94043 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
67144409 170539 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
CHEMBL4457786 170539 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cn1 10.1021/acs.jmedchem.6b01071
CHEMBL268720 209018 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44572235 188917 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 188917 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
145955182 161862 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 515 8 1 7 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccs3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4166009 161862 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 515 8 1 7 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccs3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44593425 176191 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
CHEMBL460480 176191 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmc.2008.05.024
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143135 173950 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4555444 173950 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3nccs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44365087 38613 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 452 9 3 2 7.0 Oc1ccc(CCCCNCCc2c(-c3cc(Cl)cc(Cl)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL146693 38613 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 452 9 3 2 7.0 Oc1ccc(CCCCNCCc2c(-c3cc(Cl)cc(Cl)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
67143397 171580 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 9 2 8 3.9 CNC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4473168 171580 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 9 2 8 3.9 CNC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
10074296 9298 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
CHEMBL11149 9298 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
44444642 93934 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250770 93934 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 629 8 1 6 5.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
10074296 9298 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11149 9298 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
10074296 9298 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11149 9298 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
44402469 71334 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196439 71334 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
44402463 127002 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL366236 127002 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
11720984 63149 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL179885 63149 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 555 9 3 5 4.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
11330164 64872 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182513 64872 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 540 10 1 7 4.1 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365280 120623 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(C)c1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL357622 120623 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(C)c1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
44346667 113244 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44348265 166747 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL429381 166747 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
118167818 178852 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4740373 178852 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
44444639 154428 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401193 154428 0 None - 0 Rat 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
44444672 168836 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL442283 168836 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
118178986 181617 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
CHEMBL4782882 181617 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
44444639 154428 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401193 154428 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 589 8 1 5 5.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N(C)C)CC2)c1 10.1016/j.bmcl.2007.09.099
67143773 169937 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449450 169937 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 619 8 1 8 4.8 Cc1c(N2CCN(Cc3ccc(Cl)o3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444652 94066 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251578 94066 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
162651368 179756 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 533 4 1 3 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(C(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4751238 179756 0 None - 0 Human 4.8 pIC50 = 4.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 533 4 1 3 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(C(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
162660654 180718 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4762368 180718 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
118179218 179435 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4747248 179435 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 565 5 1 4 5.1 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccc(F)c3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44593425 176191 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
CHEMBL460480 176191 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1021/jm701249f
11634198 186783 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL493344 186783 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44573111 187014 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494738 187014 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44593425 176191 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
CHEMBL460480 176191 0 None - 1 Rat 7.8 pIC50 = 7.8 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 486 5 2 6 3.7 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2009.02.043
11634198 186783 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmc.2012.09.013
CHEMBL493344 186783 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmc.2012.09.013
44293591 101125 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298700 101125 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
71449141 79088 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 483 7 2 6 6.5 CC[C@H]1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c([N+](=O)[O-])cc23)N1 10.1016/j.bmcl.2003.12.101
CHEMBL2113716 79088 0 None - 0 Rat 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 483 7 2 6 6.5 CC[C@H]1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c([N+](=O)[O-])cc23)N1 10.1016/j.bmcl.2003.12.101
11525693 69487 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL193749 69487 0 None - 0 Human 7.8 pIC50 = 7.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 8 2 7 5.6 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 211941 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL None None None None 10.1021/jm0506928
67143815 170974 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464440 170974 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 651 8 1 8 5.8 Cc1c(N2CCN(Cc3cccc4ccsc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
70691931 73840 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023088 73840 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1924 45 22 28 -1.5 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CCCCNC(C)=O)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL3085508 209243 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44402335 71272 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196337 71272 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 470 8 1 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)CC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402273 139743 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 456 7 1 7 5.8 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL380576 139743 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 456 7 1 7 5.8 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391771 165469 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL425524 165469 0 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL405438 155184 0 None - 0 Rat 5.8 pIC50 = 5.8 Binding
Ability to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligandAbility to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligand
ChEMBL 1820 46 20 18 5.7 C=CC1=C(C)c2cc1cc1[nH]c(cc3nc(cc4[nH]c(c2)c(C=C)c4C)C(C)=C3CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccccc2)NC(=O)C2CCC(=O)N2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)C2CC[C@@H](C(=O)NCC(N)=O)N2)c(CCC(=O)O)c1C 10.1021/jm020535y
44417615 141391 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 5.8 pIC50 = 5.8 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162653870 179961 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4753775 179961 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 489 4 1 4 3.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(C)(=O)=O)C2C 10.1021/acs.jmedchem.0c01076
11167850 2701 22 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
162652474 179869 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4752711 179869 0 None - 0 Human 4.7 pIC50 = 4.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 519 5 1 3 5.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(Cc1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
87285770 175470 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
CHEMBL4590493 175470 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 803 15 2 10 6.4 CCOP(=O)(O)CCCN[C@@H](Cn1c(=O)c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/acs.jmedchem.6b01071
44444673 93847 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL250389 93847 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL436874 211941 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL None None None None 10.1021/jm0506928
44573790 192659 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
CHEMBL523849 192659 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
44402469 71334 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196439 71334 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 599 13 3 9 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)C)c21 10.1016/j.bmcl.2005.03.030
67142711 171457 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccccc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4471620 171457 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3ccccc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
145957680 161548 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3C(F)(F)F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4161096 161548 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 563 7 1 6 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3C(F)(F)F)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 133819 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44417614 141086 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44359200 12099 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 509 8 2 5 6.3 CCN(CC)C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL1184288 12099 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 509 8 2 5 6.3 CCN(CC)C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL343040 12099 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 509 8 2 5 6.3 CCN(CC)C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
44388018 60152 0 None 389 2 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 60152 0 None 389 2 Human 6.7 pIC50 = 6.7 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44402649 97734 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL274002 97734 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
145948913 166925 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1276 29 16 15 -1.9 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCC1 10.1039/C5MD00259A
CHEMBL4299455 166925 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1276 29 16 15 -1.9 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCC1 10.1039/C5MD00259A
44365485 121013 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 435 9 3 3 6.2 Oc1ccc(CCCCNCCc2c(-c3cccc4cnccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL358524 121013 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 435 9 3 3 6.2 Oc1ccc(CCCCNCCc2c(-c3cccc4cnccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
15462666 96055 4 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96055 4 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346398 14369 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14369 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346398 14369 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14369 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402426 132236 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL370028 132236 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 455 8 2 7 5.1 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391849 122439 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360743 122439 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 435 7 1 4 4.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(C1CC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44391670 64361 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
CHEMBL181864 64361 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
1185 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL None None None None 10.1021/jm0506928
67143613 170459 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456703 170459 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cccnc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
1185 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44185958 154459 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401349 154459 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
10077523 122199 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL360429 122199 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44395463 126254 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL365366 126254 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 627 7 2 7 7.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCC[C@H](C(F)(F)F)N2C)cc(C)c1C 10.1016/j.bmcl.2004.08.056
44380512 57132 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Compound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assayCompound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assay
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165456 57132 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Compound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assayCompound was evaluated for the inhibition of Gonadotropin-releasing hormone receptor-stimulated [3H]inositol phosphate hydrolysis using functional assay
ChEMBL 617 9 4 4 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccc3[nH]c(O)nc3c2)c1 10.1016/s0960-894x(02)00026-4
11980076 206711 27 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm990433g
CHEMBL1007 206711 27 None - 1 Rat 8.7 pIC50 = 8.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm990433g
CHEMBL3085508 209243 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44444632 93884 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250569 93884 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 622 7 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
67143374 171175 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467261 171175 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 614 8 1 8 4.1 Cc1c(N2CCN(Cc3cncc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67144466 175207 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4583933 175207 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10032223 12097 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184284 12097 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342822 12097 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
18914263 96453 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL265774 96453 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 630 15 3 4 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293264 100744 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295908 100744 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 12 3 4 5.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44214069 100848 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL296644 100848 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 575 14 3 5 6.1 CCOC(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292838 101047 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL298074 101047 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 574 13 3 4 5.6 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
21254068 101318 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300045 101318 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 12 3 5 5.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293076 101351 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL300268 101351 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 600 12 3 4 6.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293070 165542 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL42592 165542 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 15 3 4 7.0 CCN(CC)C(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
18914272 169114 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL443768 169114 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 588 14 3 4 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
21254089 181075 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47761 181075 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44413066 77996 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 579 10 1 7 6.5 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211098 77996 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 579 10 1 7 6.5 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44412947 96313 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 608 10 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N(C)C(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL264574 96313 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 608 10 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N(C)C(=O)NC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
1184 3676 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 3676 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 3676 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to monkey recombinant LHRH receptor expressed in CHO cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
44348572 96852 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL269097 96852 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44348571 159473 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL410799 159473 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 41 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@H](NC(=O)CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44292869 176448 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL46312 176448 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)c4cnccn4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44296258 101154 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCC(C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
CHEMBL298937 101154 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 613 7 3 7 7.1 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCCC(C(F)(F)F)N2)cc(C)c1C 10.1016/j.bmcl.2003.12.101
1184 3676 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cellsTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 3676 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cellsTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 3676 31 None 426 2 Human 8.7 pIC50 = 8.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cellsTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to monkey Leutinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
44321100 106609 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL315909 106609 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 604 11 2 3 8.5 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC(CC5)C4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 209243 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
9961721 167914 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 8.7 pIC50 = 8.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44380552 58451 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168655 58451 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
44380317 167924 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL435262 167924 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2cncc3ccccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL3085508 209243 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL None None None None 10.1021/jm0506928
44293485 101045 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
CHEMBL298051 101045 0 None - 0 Rat 8.7 pIC50 = 8.7 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 590 12 1 3 8.2 CCN(CCCCc1ccncc1)CCc1c(-c2cc(C)cc(C)c2)[nH]c2ccc(C(C)(C)C(=O)N3C4CCC3CC4)cc12 10.1016/s0960-894x(01)00275-x
44402518 157980 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL409138 157980 0 None - 0 Human 8.7 pIC50 = 8.7 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
1185 3645 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
15602805 8023 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 8023 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
145962692 161706 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4163619 161706 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44359287 11530 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180743 11530 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL139993 11530 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)on4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293348 100026 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL290991 100026 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293486 186834 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL49374 186834 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 592 13 2 3 8.5 CCN(C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44292939 100932 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL297269 100932 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 508 7 4 5 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)NC4CC4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44402395 168526 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL439879 168526 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
155569451 175634 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1711 48 21 25 -3.8 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCNC(=O)CCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4593899 175634 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1711 48 21 25 -3.8 CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCNC(=O)CCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL436874 211941 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295Q
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189K
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44380212 57313 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL166843 57313 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
44348535 159878 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 39 14 17 2.0 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CCNC(C)C)cc1 10.1021/jm970024p
CHEMBL411144 159878 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 39 14 17 2.0 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)CCNC(C)C)cc1 10.1021/jm970024p
CHEMBL407619 210924 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NCC(=O)n2cc(C)c(=O)[nH]c2=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
1185 3645 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL None None None None 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44402395 168526 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL439879 168526 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1649 43 18 19 1.4 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@@H](N)CC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL407619 210924 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NCC(=O)n2cc(C)c(=O)[nH]c2=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1016/j.bmcl.2005.03.085
87285521 174447 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4567165 174447 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11167850 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44321147 162928 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL420051 162928 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 618 11 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCC5(CCCC5)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 209243 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
53239615 175292 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccco3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4585969 175292 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccco3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11167850 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL None None None None 10.1021/jm0506928
44359458 12041 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184171 12041 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336884 12041 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 545 7 3 7 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
10345138 122042 0 None 2041 2 Human 8.6 pIC50 = 8.6 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 122042 0 None 2041 2 Human 8.6 pIC50 = 8.6 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 122042 0 None 2041 2 Human 8.6 pIC50 = 8.6 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
44293335 172058 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
CHEMBL449351 172058 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 550 12 2 3 7.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1)C1CCCCC1 10.1016/s0960-894x(01)00275-x
44293487 101163 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL299006 101163 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 594 15 2 3 8.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44293803 188295 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50721 188295 0 None - 0 Rat 8.6 pIC50 = 8.6 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 564 11 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44402398 96531 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL266420 96531 0 None - 0 Human 8.6 pIC50 = 8.6 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
87285768 169927 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assayAntagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169927 1 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assayAntagonist activity against human GnRH receptor expressed in HEK293 cells assessed as reduction in ERK1/2 phosphorylation pre-incubated for 5 mins before LHRH stimulation for 5 mins by chemiluminescence based assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL3085508 209243 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203E
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203Q
ChEMBL None None None None 10.1021/jm0506928
67143420 162358 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4173938 162358 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44359471 12092 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184266 12092 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341717 12092 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 550 7 3 7 6.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)ns4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
162649425 179440 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4747322 179440 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
86275345 181488 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4781434 181488 1 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
10897903 79365 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 0 8 7.2 CCC(=O)N(C)c1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21185 79365 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 694 11 0 8 7.2 CCC(=O)N(C)c1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44274227 98436 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 654 10 0 9 6.8 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc([N+](=O)[O-])cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
CHEMBL279223 98436 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 654 10 0 9 6.8 COc1cccc(-n2c(=O)c3c(CN(C)Cc4ccccc4)c(-c4ccc([N+](=O)[O-])cc4)sc3n(Cc3c(F)cccc3F)c2=O)c1 10.1021/jm020180i
44274247 98935 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL282679 98935 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(OC)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
15895695 106471 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
CHEMBL314963 106471 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
44365771 119079 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 541 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL346195 119079 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 541 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL96693 214142 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCN)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44573628 192614 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
CHEMBL523527 192614 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 473 5 1 5 6.2 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
44417614 141086 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
67142907 169792 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447551 169792 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
10930638 98572 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44305306 100150 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 661 11 1 8 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL291893 100150 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 661 11 1 8 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccccc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
9984259 110012 0 None 281 2 Human 7.7 pIC50 = 7.7 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 110012 0 None 281 2 Human 7.7 pIC50 = 7.7 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44391752 161113 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL413062 161113 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
145958486 161634 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 541 8 1 7 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(SC)cc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4162543 161634 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 541 8 1 7 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(SC)cc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 133819 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44365459 98351 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 7 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL278496 98351 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 384 7 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365399 119168 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL347121 119168 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365457 168102 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 426 10 3 2 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL436414 168102 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 426 10 3 2 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44274228 98221 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(Cl)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL277436 98221 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(Cl)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44274229 98253 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(Cl)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL277653 98253 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2cccc(Cl)c2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44274475 98695 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2OC)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL281167 98695 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2OC)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44346397 114000 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322442 112258 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 5 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL330524 112258 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 5 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
44322433 204944 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 5 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89443 204944 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 5 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCC2CCCN2C)c1 10.1016/s0960-894x(99)00446-1
11692806 79406 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212051 79406 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11606766 79440 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccccc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212207 79440 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccccc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11512905 137890 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL377396 137890 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 628 10 2 6 7.3 CNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)C(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
44267059 8416 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 503 12 3 3 6.4 CCS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL10941 8416 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 503 12 3 3 6.4 CCS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44267091 9708 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 453 10 3 2 6.6 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11370 9708 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 453 10 3 2 6.6 CC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44267250 9080 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11021 9080 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44267233 9812 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11436 9812 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44402589 124652 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL364510 124652 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
44391826 64551 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
CHEMBL182178 64551 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
44391566 65280 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183376 65280 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
9961721 167914 0 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL435167 167914 0 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44365169 40206 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 458 12 3 4 6.1 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL148244 40206 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 458 12 3 4 6.1 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44365616 41132 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149004 41132 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44365617 42333 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 460 11 4 5 4.7 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)CCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL150041 42333 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 460 11 4 5 4.7 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)CCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
3823 49951 38 None -1 11 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 49951 38 None -1 11 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 49951 38 None -1 11 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at LH-RH receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
90663999 106347 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 709 12 3 10 3.4 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1C(=O)OCc1ccccc1 10.1021/jm00129a003
CHEMBL3144570 106347 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 709 12 3 10 3.4 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1C(=O)OCc1ccccc1 10.1021/jm00129a003
44346667 113244 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44346397 114000 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10624976 21413 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm0512894
CHEMBL131751 21413 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm0512894
11592473 77680 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 568 11 1 8 6.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNCc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL209880 77680 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 568 11 1 8 6.3 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNCc3ccccc3)c2c1=O 10.1021/jm0512894
44348358 140947 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL384385 140947 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1529 40 15 19 0.7 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)c2cnccn2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44391574 65759 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
CHEMBL183847 65759 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 445 8 1 6 4.2 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccsc1 10.1016/j.bmcl.2004.10.089
10624976 21413 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm9803673
CHEMBL131751 21413 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 492 9 1 8 4.7 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CNC)c2c1=O 10.1021/jm9803673
44365172 42453 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 8 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL150150 42453 0 None - 0 Rat 4.7 pIC50 = 4.7 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 402 8 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44406776 133819 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67142907 169792 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447551 169792 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 597 8 1 9 3.3 Cc1c(N2CCN(Cc3cnccn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118179174 181894 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4786609 181894 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
12784 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
85469632 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
CHEMBL4537788 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
118179135 181436 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4780737 181436 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
12784 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 571 8 None - 1 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
44321458 105485 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313004 105485 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 658 11 2 3 9.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCCCC5C5CCCCC54)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
11618517 186973 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
CHEMBL494554 186973 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
44573670 187100 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)s1 10.1016/j.bmcl.2009.02.043
CHEMBL495174 187100 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)s1 10.1016/j.bmcl.2009.02.043
11712618 179646 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL474992 179646 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6ncccc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44402403 71185 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196288 71185 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
44402649 97734 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL274002 97734 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 675 15 3 9 6.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCCN(C)Cc3ccccc3)c21 10.1016/j.bmcl.2005.03.030
44406776 133819 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
10919052 113020 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113020 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113244 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44267255 97696 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL273725 97696 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 383 8 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
44402670 71614 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197317 71614 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
44402673 132747 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL370414 132747 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391516 64042 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL181301 64042 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44417615 141391 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402405 140786 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 395 7 1 5 5.3 COc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL383393 140786 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 395 7 1 5 5.3 COc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391613 167712 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
CHEMBL433954 167712 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
44593415 188790 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 188790 0 None - 1 Rat 4.7 pIC50 = 4.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
67143509 169498 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4443108 169498 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143490 171043 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4465381 171043 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67144353 171657 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4474058 171657 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 673 9 1 9 4.0 Cc1c(N2CCN(Cc3cccc(S(C)(=O)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285495 171586 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)n3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4473194 171586 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)n3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44267258 96925 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL269636 96925 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 369 7 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL413854 161201 0 None - 0 Rat 7.7 pIC50 = 7.7 Binding
Ability to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligandAbility to bind to Gonadotropin-releasing hormone receptor was evaluated in vitro by displacement assay using [125I][D-Lys6]-GnRH as radioligand
ChEMBL 1810 46 21 19 4.4 C=CC1=C(C)c2cc1cc1[nH]c(cc3nc(cc4[nH]c(c2)c(C=C)c4C)C(C)=C3CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)C2CCC(=O)N2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)C2CC[C@@H](C(=O)NCC(N)=O)N2)c(CCC(=O)O)c1C 10.1021/jm020535y
91810333 178998 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
CHEMBL4741994 178998 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 7 1 4 5.4 C=CCC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCN(C(C)=O)CC2 10.1021/acs.jmedchem.0c01076
11619461 187102 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL495183 187102 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
10930638 98572 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391808 65264 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183274 65264 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 587 9 3 5 5.5 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3Cl)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44406776 133819 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.7 pIC50 = 7.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL2430897 208713 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCCCCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
56655880 73839 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
CHEMBL2023087 73839 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1841 41 22 28 -2.8 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(/C(C)=N/OCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1016/j.ejmech.2012.08.014
25193700 172711 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL452547 172711 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
10930638 98572 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44348055 168443 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL439258 168443 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](NC(=O)c2ccncc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44267042 9314 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 517 12 3 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)C(C)C)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11156 9314 0 None - 0 Rat 6.7 pIC50 = 6.7 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 517 12 3 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)C(C)C)cc2)c1 10.1016/s0960-894x(01)00134-2
44391516 64042 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL181301 64042 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 441 7 1 5 4.4 CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL409979 211045 0 None - 0 Rat 5.7 pIC50 = 5.7 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None C[C@H](NC(=O)[C@H]1CCCN1C(=O)[C@@H](CCCN=C(N)N)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(=O)OCC1c2ccccc2-c2ccccc21)C(N)=O 10.1021/jm990433g
71623059 180243 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 180243 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44406776 133819 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
155538326 171812 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3ccnc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4476330 171812 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 664 8 1 8 5.0 Cc1c(N2CCN(Cc3ccnc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162656174 180292 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4757424 180292 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44406776 133819 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL2370263 208079 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm990433g
44573713 192287 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL522202 192287 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
9961721 167914 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44359419 12105 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)no4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184330 12105 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)no4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL344688 12105 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 534 7 3 7 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)no4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293592 162340 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL417363 162340 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 496 12 2 3 6.5 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44402471 134698 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL372316 134698 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44402645 168558 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL440212 168558 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
44406776 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67143621 170737 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4460880 170737 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1cccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
44406776 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL265010 208889 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44346667 113244 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44391728 65344 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183430 65344 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391784 121812 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL359860 121812 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44346667 113244 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
86274853 115687 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
CHEMBL3358414 115687 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 662 6 1 7 4.5 N#Cc1cccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ncc(C(F)(F)F)cc4F)cc3C3(CCS(=O)(=O)CC3)C2C2CC2)c1 10.1021/ml5004469
44215908 93794 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249982 93794 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
118178976 180599 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4761024 180599 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
12784 571 8 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 571 8 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 571 8 None - 1 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
24825725 192027 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL521674 192027 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
24825725 192027 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 192027 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44572287 180221 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475660 180221 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 475 4 1 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6cccnc6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
1185 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
1185 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44293343 161663 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 545 12 4 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL416286 161663 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 545 12 4 3 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NCc4ccccc4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44406776 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67144582 175133 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4582222 175133 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 653 9 1 9 4.3 COC(=O)c1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
1185 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44417615 141391 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
1185 3645 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44346397 114000 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113244 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR L300A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44402499 69480 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
CHEMBL193689 69480 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
44391714 121621 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL359668 121621 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL4564312 212259 2 None - 0 Human 5.6 pIC50 = 5.6 Binding
Affinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000335a GNRHRAffinity On-target Cellular interaction (Mechanistic biochemical IP1 assay (CHO cells stably expressing human GnRH-R, synthetic agonist Buserelin at EC80)) EUB0000335a GNRHR
ChEMBL None None None O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)[C@@H](C1CC1)N2S(=O)(=O)c1ccc(F)cc1 nan
44346667 113244 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
1185 3645 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
10208964 66349 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
CHEMBL185438 66349 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligandBinding affinity towards human gonadotropin releasing hormone receptor expressed in CHO cells was determined by using [125I]-buserelin as radioligand
ChEMBL 536 7 2 7 7.2 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnsn4)cc3c2OCCC2CCCC2)cc(C)c1C 10.1016/j.bmcl.2004.08.056
86275345 181488 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4781434 181488 1 None - 0 Human 5.6 pIC50 = 5.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44444617 93711 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249372 93711 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 656 8 2 5 7.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N(C)C)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
71666685 182132 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4789613 182132 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
86275343 182909 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4799511 182909 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44322432 204955 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 427 6 2 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL89501 204955 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 427 6 2 6 4.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2CCN2)c1 10.1016/s0960-894x(99)00447-3
44365628 38697 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 554 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL146762 38697 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 554 10 3 5 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL264501 208877 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44365458 41628 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 8 3 2 5.9 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL149387 41628 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 8 3 2 5.9 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
87285565 169702 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446131 169702 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 679 9 1 8 5.4 Cc1c(N2CCN(Cc3cccc(OC(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11619461 187102 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL495183 187102 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
44402072 71395 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196616 71395 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 442 8 1 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391566 65280 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183376 65280 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 455 8 1 5 4.8 CCSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365251 38338 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3cc4ccccc4s3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL146484 38338 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3cc4ccccc4s3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
44214066 167772 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3ccc4ccccc4c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL434318 167772 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 434 9 3 2 6.8 Oc1ccc(CCCCNCCc2c(-c3ccc4ccccc4c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
44348357 96147 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 17 19 0.2 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2c[nH]nc2N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
77068809 96147 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 17 19 0.2 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2c[nH]nc2N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL263200 96147 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1532 40 17 19 0.2 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](NC(=O)c2c[nH]nc2N)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
162670223 181989 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4787856 181989 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
162650892 179649 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 179649 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44573112 187015 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494739 187015 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
11583756 189062 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL515123 189062 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6nccnc56)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
9961721 167914 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10930638 98572 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL436874 211941 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302Q
ChEMBL None None None None 10.1021/jm0506928
CHEMBL2430898 208714 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
67143119 175281 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4585638 175281 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 742 14 2 11 4.7 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCCCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402470 140600 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 437 8 1 6 5.5 COc1ccc(C(C)=O)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL382747 140600 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 437 8 1 6 5.5 COc1ccc(C(C)=O)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391835 165751 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL427146 165751 0 None - 0 Human 5.6 pIC50 = 5.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
11167850 2701 22 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44346397 114000 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 5.6 pIC50 = 5.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
87285554 172758 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526641 172758 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 631 8 1 7 4.8 Cc1c(N2CCN(Cc3cccc(F)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL436874 211941 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL None None None None 10.1021/jm0506928
118178983 182849 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4798682 182849 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 552 5 1 5 4.1 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1cccnc1)C2C 10.1021/acs.jmedchem.0c01076
12784 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHRAffinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
85469632 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHRAffinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
CHEMBL4537788 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Affinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHRAffinity Biochemical interaction (Tag Lite binding assay (human GnRH-R binding)) EUB0000347a GNRHR
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 nan
118167818 178852 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4740373 178852 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
44365919 120545 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 597 12 4 6 4.9 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(CC(N)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL356890 120545 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 597 12 4 6 4.9 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(CC(N)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44573626 186949 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494416 186949 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
44573627 192260 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
CHEMBL522188 192260 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 459 4 1 5 5.9 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)s1 10.1016/j.bmcl.2009.02.043
44406776 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44444628 93883 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250568 93883 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
12784 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 571 8 None - 1 Human 7.6 pIC50 = 7.6 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
9979079 8279 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL10931 8279 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
9979079 8279 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL10931 8279 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
44402472 132300 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370145 132300 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44406776 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44380192 57146 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
CHEMBL165534 57146 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 584 8 2 3 8.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCc2cccc3ncccc23)c1 10.1016/s0960-894x(02)00026-4
118074127 175144 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4582367 175144 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 714 12 2 11 3.9 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2OCC(=O)O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
87285473 173518 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4544693 173518 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 663 8 1 7 5.6 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44267251 98026 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 398 9 2 3 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cncnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL275920 98026 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 398 9 2 3 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cncnc2)c1 10.1016/s0960-894x(01)00133-0
44402589 124652 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL364510 124652 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 542 9 2 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N(C)C)c21 10.1016/j.bmcl.2005.03.030
44391612 63168 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL179977 63168 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44444663 93766 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249771 93766 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44406776 133819 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133819 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
87285768 169927 1 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169927 1 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118179051 179638 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179638 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL385022 210594 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL405176 210800 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11604354 186941 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
CHEMBL494400 186941 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
9961721 167914 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 7.6 pIC50 = 7.6 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44359331 12035 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nnc(C)s4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184148 12035 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nnc(C)s4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL334904 12035 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 551 7 3 8 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nnc(C)s4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44267036 9588 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 482 11 4 2 6.7 CCNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11299 9588 0 None - 0 Rat 7.6 pIC50 = 7.6 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 482 11 4 2 6.7 CCNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44402256 135756 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL373340 135756 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 519 8 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2005.03.030
67143633 172738 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4526188 172738 0 None - 0 Human 7.6 pIC50 = 7.6 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 612 8 2 8 3.2 Cc1c(N2CCN(Cc3ccc(=O)[nH]c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44406776 133819 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y284F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL93608 214129 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None C[C@H](NC(=O)[C@H]1CCCN1C(=O)[C@@H](CCCN=C(N)N)NC(=O)CNC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](Cc1ccccc1)NC(=O)[C@@H](N)Cc1ccc2ccccc2c1)C(N)=O 10.1021/jm990433g
44348298 81138 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL216112 81138 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2ccc(Cl)cc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44402431 71069 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 440 8 1 7 5.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195924 71069 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 440 8 1 7 5.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402378 69333 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL193529 69333 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402553 71089 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196079 71089 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
44402057 71594 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL197254 71594 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391548 65702 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183698 65702 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391728 65344 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183430 65344 0 None - 0 Rat 6.6 pIC50 = 6.6 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 532 10 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365250 121344 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 437 9 3 3 6.2 Cn1ccc2cc(-c3[nH]c4ccccc4c3CCNCCCCc3ccc(O)cc3)ccc21 10.1016/s0960-894x(00)00707-1
CHEMBL359001 121344 0 None - 0 Rat 5.6 pIC50 = 5.6 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 437 9 3 3 6.2 Cn1ccc2cc(-c3[nH]c4ccccc4c3CCNCCCCc3ccc(O)cc3)ccc21 10.1016/s0960-894x(00)00707-1
145948856 166921 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1290 29 16 15 -1.5 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCCC1 10.1039/C5MD00259A
CHEMBL4299432 166921 0 None - 0 Human 6.6 pIC50 = 6.6 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1290 29 16 15 -1.5 NC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@@H](Cc2cnc[nH]2)NC(=O)[C@@H](CO)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]cn2)NC(=O)[C@H]2CCC(=O)N2)CCCC1 10.1039/C5MD00259A
118179051 179638 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179638 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573277 186863 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493931 186863 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44346667 113244 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
15602808 8025 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 8025 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44406776 133819 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144466 175207 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4583933 175207 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 596 8 1 8 3.9 Cc1c(N2CCN(Cc3cccnc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11618517 186973 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
CHEMBL494554 186973 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 414 4 2 4 4.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]cn5)CC4)cccc3[nH]2)cc1 10.1016/j.bmcl.2009.02.043
11583388 8206 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092626 8206 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44359312 12095 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184274 12095 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL342396 12095 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
11167850 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44305286 100281 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 611 11 1 8 5.4 C=CC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
CHEMBL292773 100281 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 611 11 1 8 5.4 C=CC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00372-4
44305362 102211 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 651 11 1 9 6.1 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccoc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL304633 102211 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 651 11 1 9 6.1 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccoc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11167850 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
44380551 58450 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL168649 58450 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 612 10 2 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCc2ccc3ncccc3c2)c1 10.1016/s0960-894x(02)00026-4
44293075 90233 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL239108 90233 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 614 12 3 4 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44214108 100647 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL295152 100647 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 656 13 3 4 7.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293053 101022 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL297918 101022 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 13 3 4 6.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293054 101025 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297927 101025 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 603 14 3 5 6.8 CCOC(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292977 173665 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45489 173665 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 14 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C(C)C)C(C)C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292785 176433 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL46268 176433 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293194 185853 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
CHEMBL48763 185853 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 14 3 4 6.8 CCN(C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1)C(C)C 10.1016/s0960-894x(01)00274-8
18914248 187148 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL49542 187148 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 602 15 3 4 6.4 CCN(CC)C(=O)Cc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293074 187200 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49578 187200 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 612 12 3 4 6.7 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44292827 187605 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49891 187605 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 628 13 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(CC(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
44348401 161150 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL413456 161150 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1561 40 15 17 2.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](NC(C)=O)NC(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL436874 211941 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL None None None None 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186D
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203K
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T51A
ChEMBL None None None None 10.1021/jm0506928
67142985 172309 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3cccc(Cl)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4515452 172309 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 579 8 1 7 4.3 Cc1c(N2CCN(Cc3cccc(Cl)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44293484 96268 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL264193 96268 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 1 3 8.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)C(C)C)c1 10.1016/s0960-894x(01)00275-x
44402398 96531 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL266420 96531 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1536 41 17 18 1.6 CC(C)C[C@H](NC(=O)[C@@H](Cc1ccc(NC(N)=O)cc1)NC(=O)[C@H](Cc1ccc(NC(=O)C(N)CN)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](N)Cc1ccc2ccccc2c1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402638 160711 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL411987 160711 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL3085508 209243 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
10258659 12093 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184268 12093 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL341809 12093 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
22100905 183684 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL48380 183684 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
86275342 115686 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
CHEMBL3358413 115686 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
44341081 167501 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL432450 167501 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 590 10 2 3 8.0 CCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL3085508 209243 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111Q
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL None None None None 10.1021/jm0506928
44293511 100816 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296426 100816 0 None - 0 Rat 8.5 pIC50 = 8.5 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 538 13 2 3 7.1 CCN(CC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
11167850 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L112K
ChEMBL None None None None 10.1021/jm0506928
44572235 188917 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
CHEMBL513998 188917 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 522 4 2 6 4.4 Cn1c(=O)c(=O)[nH]c2ccc(CN3CCN(c4cccc5[nH]c(-c6ccc(C(C)(C)C)cc6)nc45)CC3)cc21 10.1021/jm801572m
44402638 160711 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL411987 160711 0 None - 0 Human 8.5 pIC50 = 8.5 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1592 43 17 18 2.2 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CCN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL436874 211941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR A50T
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL None None None None 10.1021/jm0506928
44359333 11525 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180707 11525 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138999 11525 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293617 188090 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50380 188090 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 522 10 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C(C)CCC4C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44380148 119805 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
CHEMBL352782 119805 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptorInhibition of [125I]buserelin binding to human pituitary gonadotropin-releasing hormone receptor
ChEMBL 626 11 2 3 9.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNCCCCc2ccc3cnccc3c2)c1 10.1016/s0960-894x(02)00026-4
11167850 2701 22 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K191E
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR T190K
ChEMBL None None None None 10.1021/jm0506928
87285732 172383 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4517137 172383 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL3085508 209243 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168I
ChEMBL None None None None 10.1021/jm0506928
67143598 170074 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4451280 170074 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44359191 12100 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184298 12100 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL343396 12100 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ccncc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL436874 211941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S124A
ChEMBL None None None None 10.1021/jm0506928
44293284 183503 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 8 5.9 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
CHEMBL48249 183503 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 543 7 3 8 5.9 O=C(Nc1ccncn1)c1cc2c(OCC[C@@H]3CCCCN3)c(-c3ccc(Cl)s3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00318-8
11478448 65745 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183779 65745 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
15462663 98590 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(OC)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL280350 98590 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 639 10 0 8 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccc(OC)cc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44365612 40583 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 610 12 3 5 6.8 CCCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL148571 40583 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 610 12 3 5 6.8 CCCC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44365627 41399 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 582 10 3 5 6.0 CC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL149188 41399 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 582 10 3 5 6.0 CC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44365595 42285 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 485 10 4 4 6.0 CNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL149992 42285 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 485 10 4 4 6.0 CNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
44292785 176433 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL46268 176433 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 499 10 3 4 6.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44365865 193127 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 513 12 4 4 6.8 CCCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL538660 193127 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 513 12 4 4 6.8 CCCNC(=O)Oc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
44444670 94043 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251388 94043 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCCC(O)C3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444678 154400 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401081 154400 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
44417614 141086 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
9917213 201717 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 627 11 1 8 5.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL65569 201717 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 627 11 1 8 5.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11642933 77756 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210277 77756 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44412946 77761 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 656 11 2 7 8.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)Nc4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL210295 77761 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 656 11 2 7 8.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(NC(=O)Nc4ccccc4)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
70697569 77620 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL2096778 77620 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.6 CC(C)(C)CNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44365252 37566 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3csc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL145840 37566 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 9 3 3 6.9 Oc1ccc(CCCCNCCc2c(-c3csc4ccccc34)[nH]c3ccccc23)cc1 10.1016/s0960-894x(00)00707-1
44322402 204480 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL86490 204480 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.6 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
44322443 204768 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 3 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL88293 204768 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 3 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OC2CCCN(C)CC2)c1 10.1016/s0960-894x(99)00446-1
9873394 79509 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 596 12 0 8 7.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(CC)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL212472 79509 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 596 12 0 8 7.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(CC)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11635837 138558 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccc(OC)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL378654 138558 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccc(OC)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11527301 138699 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2cccc(F)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL378845 138699 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2cccc(F)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44267057 8257 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 411 9 3 2 6.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL10929 8257 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 411 9 3 2 6.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)cc2)c1 10.1016/s0960-894x(01)00134-2
44267073 9145 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 414 9 2 1 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(F)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11067 9145 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 414 9 2 1 6.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(F)cc2)c1 10.1016/s0960-894x(01)00134-2
44267029 9157 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 551 12 3 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)c3ccccc3)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11074 9157 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 551 12 3 3 7.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(=O)(=O)c3ccccc3)cc2)c1 10.1016/s0960-894x(01)00134-2
44402105 124283 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL364246 124283 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
44391499 65602 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183600 65602 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365598 41402 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149189 41402 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44365351 121489 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL359370 121489 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 462 11 4 6 4.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC[C@H](O)COc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
15462666 96055 4 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96055 4 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44365028 42224 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 457 10 3 4 5.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC(=O)CCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149940 42224 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 457 10 3 4 5.1 COc1ccc(-c2[nH]c3ccccc3c2CCNC(=O)CCCc2ccc(N)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44214065 120554 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 534 14 2 4 7.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(OCc3ccccc3)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL356970 120554 0 None - 0 Rat 4.5 pIC50 = 4.5 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 534 14 2 4 7.6 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(OCc3ccccc3)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
162667361 181943 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
CHEMBL4787218 181943 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
162675445 182826 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4798298 182826 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL428186 211677 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N(C)CC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44573586 186918 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494232 186918 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
44346667 113244 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10930638 98572 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402466 71541 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197089 71541 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44573713 192287 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
CHEMBL522202 192287 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)n(C)n1 10.1016/j.bmcl.2009.02.043
44391754 168108 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL436472 168108 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL436874 211941 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL None None None None 10.1021/jm0506928
162650892 179649 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 179649 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
9982147 204566 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
CHEMBL87020 204566 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
44365644 41390 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 612 11 3 6 6.6 CCOC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL149181 41390 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 612 11 3 6 6.6 CCOC(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
44365772 42142 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 539 10 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL149881 42142 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 539 10 3 4 7.3 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCCCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
44561397 189232 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 189232 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44359301 11531 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180754 11531 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141221 11531 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 537 7 3 8 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nncs4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44358957 12038 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184158 12038 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL336039 12038 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 530 7 3 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cccnc4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44293130 181310 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL47791 181310 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(N)=O)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293131 188252 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL50663 188252 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 520 10 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4C5CCC4CC5)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44214072 176844 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 484 11 3 4 6.5 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL46385 176844 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 484 11 3 4 6.5 CCOC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
9982147 204566 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL87020 204566 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
44406776 133819 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44573625 186948 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494415 186948 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
44359303 11532 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1180760 11532 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL141539 11532 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 520 7 4 7 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4nc[nH]n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44391714 121621 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL359668 121621 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccncc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44402571 124433 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL364297 124433 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1ccccc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391498 165567 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL426060 165567 0 None - 0 Rat 5.5 pIC50 = 5.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
67144370 174043 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4557575 174043 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3cccc(F)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143547 170950 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4464132 170950 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccc(C#N)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11626096 186687 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
CHEMBL492780 186687 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
44444678 154400 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401081 154400 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 618 12 1 5 7.3 CCN(CC)CCOC1CCN(CCc2c(-c3cc(C)cc(C)c3)[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc23)CC1 10.1016/j.bmcl.2007.09.099
11620431 178789 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL473807 178789 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 509 4 3 6 3.8 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cnc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
11671279 130362 0 None 331 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 130362 0 None 331 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44402492 125663 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
CHEMBL364933 125663 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1cccnc1 10.1016/j.bmcl.2005.03.030
44402471 134698 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL372316 134698 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 485 9 2 7 6.0 CCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391548 65702 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183698 65702 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 8 1 5 5.3 CCSc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44561105 186169 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 476 6 3 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL488812 186169 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 476 6 3 5 4.7 FC(F)(F)c1nc2c(N3CCN(CCCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44417615 141391 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346398 14369 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14369 0 None - 1 Human 5.5 pIC50 = 5.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402572 70850 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 2 7 4.6 CNC(=O)Nc1ccc2c(c1)nc(SCc1cc([N+](=O)[O-])ccc1OC)n2C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195626 70850 0 None - 0 Human 5.5 pIC50 = 5.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 429 7 2 7 4.6 CNC(=O)Nc1ccc2c(c1)nc(SCc1cc([N+](=O)[O-])ccc1OC)n2C(C)C 10.1016/j.bmcl.2005.03.030
44444647 154462 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL401352 154462 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 688 10 2 7 4.6 CC(=O)N1CCN(CC(O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
44444676 154399 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401080 154399 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 9 1 6 5.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(OCC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
118179235 181353 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4779806 181353 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
118179051 179638 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179638 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573110 186611 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL492327 186611 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44577104 178169 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL468565 178169 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
11294792 62958 0 None 380 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 62958 0 None 380 2 Human 7.5 pIC50 = 7.5 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
67143679 173589 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 544 8 1 6 4.8 Cc1c(N2CCC(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4546864 173589 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 544 8 1 6 4.8 Cc1c(N2CCC(Cc3ccccc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143755 174853 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4576169 174853 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44391826 64551 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
CHEMBL182178 64551 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 549 10 3 6 4.2 COc1ccc(CNS(=O)(=O)c2ccc3c(c2)nc(CCNC(=O)NC(C)(C)C)n3Cc2ccccc2)cc1 10.1016/j.bmcl.2004.10.090
44444645 154461 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL401351 154461 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 672 9 2 6 4.8 CC(=O)NC1CCN(C(=O)CN2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
162665107 181554 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4782228 181554 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
44444626 154344 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL400739 154344 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
44402464 168523 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL439860 168523 0 None - 0 Rat 7.5 pIC50 = 7.5 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 211941 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL None None None None 10.1021/jm0506928
67143749 169579 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 561 8 2 8 3.4 Cc1c(N2CCN(Cc3ccc(O)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4444237 169579 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 561 8 2 8 3.4 Cc1c(N2CCN(Cc3ccc(O)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143490 171043 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4465381 171043 0 None - 0 Human 7.5 pIC50 = 7.5 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cscn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
11525358 186759 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
CHEMBL493185 186759 0 None - 0 Rat 6.5 pIC50 = 6.5 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
44417615 141391 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402360 132922 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 505 7 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1-c1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL370623 132922 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 505 7 2 7 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1-c1ccccc1 10.1016/j.bmcl.2005.03.030
67143710 169768 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4447139 169768 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 620 8 1 8 4.4 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
9979079 8279 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL10931 8279 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibition of human Gonadotropin-releasing hormone receptor bindingInhibition of human Gonadotropin-releasing hormone receptor binding
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00134-2
9979079 8279 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL10931 8279 0 None - 0 Human 6.5 pIC50 = 6.5 Binding
Inhibitory activity evaluated against human Gonadotropin-releasing hormone receptorInhibitory activity evaluated against human Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00133-0
162660654 180718 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4762368 180718 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 539 5 1 5 4.2 O=C(Nc1ccc2c(c1)C1(CC[S+]([O-])CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44322400 204560 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCCN2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL86976 204560 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 2 6 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCCCCN2)c1 10.1016/s0960-894x(99)00447-3
44322420 204968 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 5 2 6 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00447-3
CHEMBL89672 204968 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 441 5 2 6 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00447-3
44293274 100786 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL296199 100786 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 510 12 1 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCN(C)CCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293594 101096 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL298497 101096 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 512 13 3 4 5.5 CCN(CCO)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccncc3)c2c1 10.1016/s0960-894x(01)00275-x
44293134 186818 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL49366 186818 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 604 12 2 3 7.6 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(F)(F)F)CC(F)(F)F)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44348278 156337 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2cccnc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL407193 156337 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C(=O)c2cccnc2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44267048 162669 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 475 10 3 3 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(S(N)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL418339 162669 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 475 10 3 3 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(S(N)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
44267256 9074 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 447 9 2 2 7.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cnc3ccccc3c2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11014 9074 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 447 9 2 2 7.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cnc3ccccc3c2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL2430900 208716 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma countingDisplacement of [125I]-[DTrp6]-LH-RH from human GnRH receptor after 3 hrs by gamma counting
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNC(=O)CCCCCNC(=O)CN1CCN(CC(=O)O)CCN(CC(=O)O)CCN(CC(=O)O)CC1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.bmcl.2013.08.075
67143674 174497 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccc([N+](=O)[O-])cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4568223 174497 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3ccc([N+](=O)[O-])cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44402105 124283 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
CHEMBL364246 124283 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 533 9 2 7 6.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1CCc1ccccc1 10.1016/j.bmcl.2005.03.030
44346397 114000 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162645007 178881 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573625 186948 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494415 186948 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
15602806 8212 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 8212 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44402553 71089 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196079 71089 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 529 9 2 9 5.4 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)OC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 211941 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL None None None None 10.1021/jm0506928
CHEMBL330173 209584 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
10919052 113020 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113020 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44444668 153745 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL398648 153745 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 6 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(=O)CN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143804 172625 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4522657 172625 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 724 13 3 9 4.1 Cc1c(N2CCN(Cc3cccc(C(=O)NCCCC(=O)O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118179169 179346 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4746174 179346 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44328354 96707 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 980 24 9 10 0.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
CHEMBL267986 96707 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL 980 24 9 10 0.4 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11518185 187105 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL495190 187105 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
10930638 98572 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391734 122103 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360297 122103 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44406776 133819 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
10919052 113020 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113020 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 141086 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10919052 113020 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113020 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391692 63969 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181057 63969 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
25194091 188423 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL508898 188423 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 498 7 3 5 5.5 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44322502 205247 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 390 4 1 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(C)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL91311 205247 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 390 4 1 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(C)ccc3c2OCC2CCCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
44309572 202636 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
CHEMBL71561 202636 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 517 7 3 7 5.4 Cc1cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4ncccn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(02)00370-0
44352512 116796 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
CHEMBL339636 116796 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 483 7 3 7 4.7 Cc1cc(-c2c(O)nc3ccc(C(=O)Nc4ccncn4)cc3c2OCC[C@@H]2CCN2)cc(C)c1C 10.1016/s0960-894x(01)00779-x
10484172 98584 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 632 12 3 6 5.8 CCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL280296 98584 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 632 12 3 6 5.8 CCS(=O)(=O)N1CCN(C(=O)Oc2ccc3[nH]c(-c4cc(C)cc(C)c4)c(CCNCCCCc4ccc(O)cc4)c3c2)CC1 10.1016/s0960-894x(00)00708-3
CHEMBL436874 211941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL None None None None 10.1021/jm0506928
10649568 14397 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of binding to GnRH receptor in ratIn vitro inhibition of binding to GnRH receptor in rat
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14397 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
In vitro inhibition of binding to GnRH receptor in ratIn vitro inhibition of binding to GnRH receptor in rat
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
10649568 14397 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of Rat gonadotropin-releasing hormone receptorInhibition of Rat gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
CHEMBL120432 14397 0 None -10 2 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of Rat gonadotropin-releasing hormone receptorInhibition of Rat gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm049218c
9936667 100052 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL291201 100052 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 525 10 3 4 5.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCOCC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44293071 101130 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL298748 101130 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 589 14 3 5 6.6 CCOC(=O)C(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293208 170577 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL445848 170577 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292988 181859 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47862 181859 0 None - 0 Rat 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 586 12 3 4 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N4CCCC4)cc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
1184 3676 31 None 426 2 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 3676 31 None 426 2 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 3676 31 None 426 2 Human 8.4 pIC50 = 8.4 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
10603202 168037 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL435974 168037 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor (LHRH) receptor.
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
1184 3676 31 None -426 2 Rat 8.4 pIC50 = 8.4 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
9874838 3676 31 None -426 2 Rat 8.4 pIC50 = 8.4 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL71917 3676 31 None -426 2 Rat 8.4 pIC50 = 8.4 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL3085508 209243 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S186K
ChEMBL None None None None 10.1021/jm0506928
67142818 173475 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4543788 173475 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccccc3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
11478448 65745 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183779 65745 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 553 9 3 5 4.9 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(Cl)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
1185 3645 32 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
15602804 7998 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 7998 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44321496 105483 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
CHEMBL312995 105483 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 657 13 2 5 6.3 CCS(=O)(=O)N1CCN(C(=O)C(C)(C)c2ccc3[nH]c(-c4cc(C)cc(C)c4)c([C@H](C)CNCCCCc4ccncc4)c3c2)CC1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 211941 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F272L
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.4 pIC50 = 8.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44341080 110089 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL325417 110089 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 604 11 2 3 8.4 CCCc1cc(CCNC[C@@H](C)c2c(-c3cc(C)cc(C)c3)[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc23)ccn1 10.1016/s0960-894x(02)00751-5
CHEMBL436874 211941 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293N
ChEMBL None None None None 10.1021/jm0506928
44321291 204554 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL86950 204554 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 632 11 2 3 9.3 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5(C)CC4CC(C)(C)C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
44321292 204563 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL87000 204563 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 590 11 2 3 8.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCCC4C5)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 211941 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL None None None None 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L117A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44293804 101329 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300095 101329 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
44593424 175559 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 175559 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL436874 211941 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL None None None None 10.1021/jm0506928
44593424 175559 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 175559 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
71623059 180243 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 180243 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44365898 119151 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 442 10 3 3 6.3 COc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
CHEMBL346903 119151 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 442 10 3 3 6.3 COc1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(00)00708-3
44593424 175559 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459215 175559 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44593424 175559 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL459215 175559 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)[nH]c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44346397 114000 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
9961721 167914 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
9961721 167914 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 7.4 pIC50 = 7.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44358962 12037 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL1184155 12037 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL335764 12037 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 559 7 3 7 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cc(C)nc(C)n4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
44267238 96072 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL262715 96072 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44413009 79355 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 537 9 1 7 6.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211808 79355 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 537 9 1 7 6.2 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44266961 9069 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 518 13 4 3 5.9 CCNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11011 9069 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 518 13 4 3 5.9 CCNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44267238 96072 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL262715 96072 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44365269 39628 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1ccc(C)c(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL147740 39628 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1ccc(C)c(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44274327 81771 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 589 10 0 7 6.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(CC(C)C)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21704 81771 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 589 10 0 7 6.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(CC(C)C)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
15462660 82414 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 623 10 0 7 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(Cc2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21804 82414 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 623 10 0 7 6.9 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(Cc2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
10930638 98572 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10930638 98572 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346397 114000 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
11527384 77137 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2cccc(OC)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL208714 77137 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2cccc(OC)c2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11226884 77315 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccc(F)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL208904 77315 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 570 10 0 7 6.7 CCOC(=O)c1cn(Cc2ccc(F)cc2)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
71459964 79087 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 573 10 2 5 7.7 Cc1cc(C)cc(-c2c(OCC[C@@H]3CCC[C@H](CCCc4ccccc4)N3)c3cc([N+](=O)[O-])c(Cl)cc3[nH]c2=O)c1 10.1016/j.bmcl.2003.12.101
CHEMBL2113713 79087 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 573 10 2 5 7.7 Cc1cc(C)cc(-c2c(OCC[C@@H]3CCC[C@H](CCCc4ccccc4)N3)c3cc([N+](=O)[O-])c(Cl)cc3[nH]c2=O)c1 10.1016/j.bmcl.2003.12.101
44391784 121812 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL359860 121812 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.9 CC(C)(C)NC(=O)CCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44365171 38594 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 416 9 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL146678 38594 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 416 9 3 4 4.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44417614 141086 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10919052 113020 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113020 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR M24I mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322380 204801 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.0 CN1CCCC(COc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
CHEMBL88516 204801 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.0 CN1CCCC(COc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
44322302 204930 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89332 204930 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 410 4 1 4 5.7 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCCN2C)c1 10.1016/s0960-894x(99)00446-1
44391510 122424 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360693 122424 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
67143420 162358 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4173938 162358 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 590 9 1 9 3.6 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
145948911 166923 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1304 29 16 15 -1.1 NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1 10.1039/C5MD00259A
CHEMBL4299453 166923 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1304 29 16 15 -1.1 NC(=O)CNC(=O)[C@@H]1CCCN1C(=O)[C@@H](Cc1ccc(O)cc1)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(=O)C1(NC(=O)[C@H](Cc2cnc[nH]2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1 10.1039/C5MD00259A
86275342 115686 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
CHEMBL3358413 115686 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/ml5004469
118179051 179638 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179638 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
11634198 186783 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL493344 186783 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44267278 9220 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 3 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)nc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11101 9220 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 3 5.6 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(N)nc2)c1 10.1016/s0960-894x(01)00133-0
44402645 168558 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL440212 168558 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 528 9 3 8 4.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC)c21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 211941 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL None None None None 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44402646 132913 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370587 132913 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
87285550 173756 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4550720 173756 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 775 13 3 9 5.4 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCP(=O)(O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
71668147 179410 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4746969 179410 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 637 6 1 6 4.6 O=C(NCc1ccc(C(F)(F)F)cn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
67143723 174826 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 8 3.8 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4575491 174826 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 8 3.8 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL406243 210853 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NC1(C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)CCC1 10.1021/jm990433g
44402463 127002 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL366236 127002 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 7 2 7 5.2 CCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL436874 211941 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302A
ChEMBL None None None None 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
118178986 181617 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
CHEMBL4782882 181617 0 None - 0 Human 6.4 pIC50 = 6.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 4 4.5 CC(=O)N1CCC2(CC1)CN(S(=O)(=O)c1ccc(F)cc1)c1ccc(C(=O)NCc3ccccc3Cl)cc12 10.1021/acs.jmedchem.0c01076
11167850 2701 22 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24IDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24I
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
86272223 115688 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
CHEMBL3358415 115688 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
11525358 186759 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
CHEMBL493185 186759 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
44444675 154184 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399857 154184 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
44402293 71084 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
CHEMBL196040 71084 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
86275345 181488 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4781434 181488 1 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
15602808 8025 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091580 8025 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5cnc6ccccc6n5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44417615 141391 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113244 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
162649425 179440 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4747322 179440 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 555 5 1 6 3.9 O=C(Nc1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL327359 209545 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCC(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44359224 11524 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 10 2 5 7.8 CCC(C)N(C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl)C(C)CC 10.1016/s0960-894x(00)00024-x
CHEMBL1180706 11524 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 10 2 5 7.8 CCC(C)N(C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl)C(C)CC 10.1016/s0960-894x(00)00024-x
CHEMBL138977 11524 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 565 10 2 5 7.8 CCC(C)N(C(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl)C(C)CC 10.1016/s0960-894x(00)00024-x
44293165 101223 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
CHEMBL299392 101223 0 None - 0 Human 7.4 pIC50 = 7.4 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 556 16 2 5 5.7 COCCN(CCOC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3cccnc3)c2c1 10.1016/s0960-894x(01)00275-x
44267275 97687 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 490 11 3 4 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)nc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL273625 97687 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 490 11 3 4 5.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)nc2)c1 10.1016/s0960-894x(01)00133-0
44295820 101515 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCCC2C)c1 10.1016/j.bmcl.2003.12.101
CHEMBL301501 101515 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCCC2C)c1 10.1016/j.bmcl.2003.12.101
44402467 170089 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL445143 170089 0 None - 0 Rat 7.4 pIC50 = 7.4 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL410269 211063 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@H](Cc1ccccc1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
11518185 187105 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL495190 187105 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 4 1 5 5.2 Cc1nn(C)c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44346397 114000 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44267254 9189 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11087 9189 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 397 9 2 2 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccccn2)c1 10.1016/s0960-894x(01)00133-0
44267271 9714 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 386 9 3 2 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2c[nH]cn2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11375 9714 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 386 9 3 2 5.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2c[nH]cn2)c1 10.1016/s0960-894x(01)00133-0
11318649 64023 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181257 64023 0 None - 0 Rat 6.4 pIC50 = 6.4 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44561142 186121 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4ccc5[nH]c(=S)[nH]c5c4)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL488478 186121 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4ccc5[nH]c(=S)[nH]c5c4)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44346397 114000 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 5.4 pIC50 = 5.4 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F313L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44267242 9957 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11523 9957 0 None - 0 Rat 5.4 pIC50 = 5.4 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44573791 186805 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493565 186805 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
145950097 162252 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 8 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4172391 162252 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 527 8 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44406776 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
118178976 180599 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4761024 180599 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 595 6 1 4 5.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44573789 186757 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493167 186757 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.8 CCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
15602807 8136 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 8136 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44572236 171333 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 171333 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44267035 96763 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 504 12 4 3 5.5 CNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL268479 96763 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 504 12 4 3 5.5 CNS(=O)(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
44402499 69480 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
CHEMBL193689 69480 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccncc1 10.1016/j.bmcl.2005.03.030
44406776 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 3645 32 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44391499 65602 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183600 65602 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 439 8 1 5 4.1 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
162647697 179279 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4745391 179279 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 523 5 1 5 5.2 O=C(Nc1ccc2c(c1)C1(CCSCC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
53239184 169034 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436375 169034 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44267054 9702 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 468 10 4 2 6.4 CNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
CHEMBL11368 9702 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 468 10 4 2 6.4 CNC(=O)Nc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cc1 10.1016/s0960-894x(01)00134-2
67144478 169783 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccc(F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4447332 169783 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 563 8 1 7 3.8 Cc1c(N2CCN(Cc3ccc(F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44406776 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290F
ChEMBL None None None None 10.1021/jm0506928
90663998 106346 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 787 14 4 10 4.9 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](CC1=CNCN1)NC(=O)[C@@H]1CCCN1C(=O)OCC(c1ccccc1)c1ccccc1 10.1021/jm00129a003
CHEMBL3144569 106346 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 787 14 4 10 4.9 O=C(NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1)[C@H](CC1=CNCN1)NC(=O)[C@@H]1CCCN1C(=O)OCC(c1ccccc1)c1ccccc1 10.1021/jm00129a003
44417615 141391 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR N27A mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44387961 165468 0 None 144 2 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 165468 0 None 144 2 Human 6.3 pIC50 = 6.3 Binding
Inhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cellsInhibition of human GnRH receptor stimulated inositol phosphate accumulation in RBL cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44391510 122424 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360693 122424 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3cccc(OC)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
162667361 181943 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
CHEMBL4787218 181943 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 468 5 1 3 5.1 CC1N(S(=O)(=O)c2ccccc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C1(C)C 10.1021/acs.jmedchem.0c01076
162645007 178881 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573791 186805 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493565 186805 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 6.2 CCCCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44573276 186833 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493731 186833 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
11226753 63014 0 None 389 2 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 63014 0 None 389 2 Human 7.3 pIC50 = 7.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
44406776 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N315D
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
87285708 173333 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4540232 173333 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 749 13 2 8 6.1 Cc1c(N2CCN(Cc3cccc(C(F)(F)F)c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
145957335 161755 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 519 7 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)C3CCSCC3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4164417 161755 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 519 7 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)C3CCSCC3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44402646 132913 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370587 132913 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 570 9 3 8 6.1 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NC(C)(C)C)c21 10.1016/j.bmcl.2005.03.030
44391628 65541 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183572 65541 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44391754 168108 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL436472 168108 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 519 9 3 5 4.2 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
53239184 169034 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4436375 169034 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 652 8 1 9 5.2 Cc1c(N2CCN(Cc3nc4ccccc4s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444641 154430 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401212 154430 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 7 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143715 172916 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4530350 172916 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3cccc(C#N)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44305604 201724 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 625 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C4CC4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL65614 201724 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 625 11 1 8 5.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)C4CC4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
11282957 121819 0 None 1096 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 121819 0 None 1096 2 Human 8.3 pIC50 = 8.3 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
44292919 100676 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL295376 100676 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44293305 100991 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL297703 100991 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 536 11 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCCC4)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44292990 100728 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL295731 100728 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 616 16 3 4 7.2 CCCN(CCC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293178 100952 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL297430 100952 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 658 17 3 4 7.9 CCCN(CCC)C(=O)C(C)(C)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44292979 187606 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL49893 187606 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 483 10 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44348173 169913 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 39 15 17 1.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL444903 169913 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1533 39 15 17 1.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](NC(C)=O)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
67143432 171561 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4472942 171561 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
11526254 187030 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 504 5 1 7 4.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccnc(S(C)(=O)=O)n5)CC4)cccc3[nH]2)cc1 10.1021/jm701249f
CHEMBL494797 187030 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 504 5 1 7 4.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccnc(S(C)(=O)=O)n5)CC4)cccc3[nH]2)cc1 10.1021/jm701249f
CHEMBL3085508 209243 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44321695 105501 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
CHEMBL313086 105501 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 592 9 2 4 6.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2cccn(C)c2=O)c1 10.1016/s0960-894x(01)00512-1
CHEMBL3085508 209243 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44348310 157279 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
CHEMBL408335 157279 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)N(C)C(=O)c2ccc(NC(C)=O)cc2)cc1 10.1021/jm970024p
155531714 175617 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175617 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
44406776 133819 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E111A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL None None None None 10.1021/jm0506928
145952094 162355 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 523 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(C)cc3C)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4173914 162355 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 523 7 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccc(C)cc3C)c2=O)c1F 10.1016/j.ejmech.2017.12.095
86275573 115689 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
CHEMBL3358416 115689 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
44561397 189232 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL516479 189232 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 458 4 3 5 3.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
11167850 2701 22 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44348418 96197 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL263629 96197 0 None - 0 Rat 8.3 pIC50 = 8.3 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1559 41 13 16 3.5 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@@H](NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(C)=O)N(C)C=O)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
44321510 106655 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL316159 106655 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 608 15 2 3 9.0 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 211941 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL None None None None 10.1021/jm0506928
44572236 171333 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL446978 171333 0 None - 0 Human 8.3 pIC50 = 8.3 Binding
Displacement of [D-Trp6]-GnRH from human recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from human recombinant GnRH receptor
ChEMBL 599 6 2 7 5.3 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6[nH]c(=O)c(=O)n(Cc7cccnc7)c6c5)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44561369 189874 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 189874 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL436874 211941 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293A
ChEMBL None None None None 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
15602805 8023 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
CHEMBL1091579 8023 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 486 5 1 7 3.5 CCn1cc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(=O)[nH]c1=O 10.1016/j.bmcl.2010.02.099
44292888 174206 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL45614 174206 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the presence of 0.1% bovine serum albumin.
ChEMBL 567 14 3 3 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44295630 190234 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 8 3 7 6.6 CCC1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc23)N1 10.1016/j.bmcl.2003.12.101
CHEMBL51841 190234 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptorInhibitory concentration against binding of [125I]buserelin to human Gonadotropin-releasing hormone receptor
ChEMBL 559 8 3 7 6.6 CCC1CCC[C@@H](CCOc2c(-c3cc(C)cc(C)c3)c(O)nc3cc(Cl)c(C(=O)Nc4ccncn4)cc23)N1 10.1016/j.bmcl.2003.12.101
CHEMBL436874 211941 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL None None None None 10.1021/jm0506928
24825725 192027 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL521674 192027 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL436874 211941 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL None None None None 10.1021/jm0506928
9979079 8279 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL10931 8279 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
15462657 79813 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 609 9 0 7 6.8 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21373 79813 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 609 9 0 7 6.8 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
9979079 8279 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL10931 8279 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
25193798 169631 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL444509 169631 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
9961721 167914 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
9979079 8279 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL10931 8279 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 412 9 3 2 6.3 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(01)00274-8
44267231 9505 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11253 9505 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 411 10 2 2 6.4 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00133-0
44391735 121823 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
CHEMBL359914 121823 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
CHEMBL436874 211941 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306A
ChEMBL None None None None 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y283F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44365420 40979 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccccc1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL148884 40979 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccccc1-c1[nH]c2ccccc2c1CCNCCCCc1ccc(O)cc1 10.1016/s0960-894x(00)00707-1
90663997 106345 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 849 14 6 11 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1=CNCN1)C(=O)NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1 10.1021/jm00129a003
CHEMBL3144568 106345 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Binding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligandBinding affinity at Leutinizing releasing hormone receptor in rat pituitary using [125I]leuprolide as radioligand
ChEMBL 849 14 6 11 4.0 CC(C)(C)OC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1=CNCN1)C(=O)NC[C@H]1CO[C@](Cn2ccnc2)(c2ccc(Cl)cc2Cl)O1 10.1021/jm00129a003
44417614 141086 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10919052 113020 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113020 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44322401 106068 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 2 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL314147 106068 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 2 4 5.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCCNC2)c1 10.1016/s0960-894x(99)00446-1
44322444 204906 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 1 4 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL89186 204906 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 396 4 1 4 5.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC2CCN(C)C2)c1 10.1016/s0960-894x(99)00446-1
11570616 77903 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 506 9 0 8 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)C)c2c1=O 10.1021/jm0512894
CHEMBL210845 77903 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 506 9 0 8 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)C)c2c1=O 10.1021/jm0512894
44412978 79348 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL211752 79348 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44267086 97626 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 441 10 2 3 6.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL273296 97626 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 441 10 2 3 6.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)c1 10.1016/s0960-894x(01)00134-2
10603202 168037 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL435974 168037 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 573 9 1 7 6.4 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
44365118 41308 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 473 12 2 5 5.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL149124 41308 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 473 12 2 5 5.9 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc([N+](=O)[O-])cc2)cc1OC 10.1016/s0960-894x(00)00707-1
11167850 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44346398 14369 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14369 0 None - 1 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417615 141391 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
11511860 138804 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 476 8 0 7 5.1 CCOC(=O)c1cn(C)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL379274 138804 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 476 8 0 7 5.1 CCOC(=O)c1cn(C)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
11167850 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44573113 192635 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
CHEMBL523711 192635 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nc1C 10.1016/j.bmcl.2009.02.043
44444665 93767 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249772 93767 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444652 94066 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL251578 94066 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 588 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44402466 71541 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197089 71541 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44391693 63436 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL180167 63436 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67144162 174481 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 657 9 1 8 4.3 Cc1c(N2CCN(Cc3cccc([S+](C)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4567854 174481 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 657 9 1 8 4.3 Cc1c(N2CCN(Cc3cccc([S+](C)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402403 71185 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
CHEMBL196288 71185 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 515 9 3 8 5.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)O)c21 10.1016/j.bmcl.2005.03.030
44561141 192897 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL527422 192897 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44346397 114000 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346667 113244 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL332355 113244 0 None - 1 Human 7.3 pIC50 = 7.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL436874 211941 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL None None None None 10.1021/jm0506928
87285768 169927 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169927 1 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
25193700 172711 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL452547 172711 0 None - 0 Rat 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 534 7 2 5 5.9 CCc1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
11167850 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 5.3 pIC50 = 5.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44417615 141391 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 5.3 pIC50 = 5.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309Q mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
87285521 174447 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4567165 174447 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3cccnc3Cl)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444644 154460 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401350 154460 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
67143487 170196 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 662 9 1 9 5.2 Cc1c(N2CCN(Cc3cccc(-c4ncco4)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4452636 170196 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 662 9 1 9 5.2 Cc1c(N2CCN(Cc3cccc(-c4ncco4)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
123549935 178854 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4740379 178854 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 551 5 1 4 4.7 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccccc1)C2C 10.1021/acs.jmedchem.0c01076
162672599 182425 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4793643 182425 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 481 4 1 5 4.1 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(NC(=O)c3cccnc3)cc2C12CCOCC2 10.1021/acs.jmedchem.0c01076
44391703 167938 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
CHEMBL435334 167938 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
162665107 181554 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4782228 181554 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 570 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ncccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
10919052 113020 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113020 0 None - 1 Human 6.3 pIC50 = 6.3 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302N mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44391526 122091 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360244 122091 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
86275342 115686 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL3358413 115686 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 671 6 1 6 5.3 O=C(NCc1ncc(Cl)cc1C(F)(F)F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44402465 134712 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL372455 134712 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
44391821 65250 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183197 65250 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67143432 171561 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4472942 171561 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 610 8 1 8 4.3 Cc1ncccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
127037454 136940 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1250 31 17 15 -2.5 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
CHEMBL3753755 136940 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1250 31 17 15 -2.5 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
9918188 154183 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399856 154183 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 708 8 2 5 8.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)C2)c1 10.1016/j.bmcl.2007.09.099
44444649 154466 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401418 154466 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44293164 167268 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL430763 167268 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 482 11 3 3 6.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)NC(C)C)cc3c2CCNCCCCc2cccnc2)c1 10.1016/s0960-894x(01)00275-x
44402670 71614 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
CHEMBL197317 71614 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 557 11 4 9 4.3 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCN)c21 10.1016/j.bmcl.2005.03.030
CHEMBL318127 209465 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CCCCN)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44573626 186949 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494416 186949 0 None - 0 Rat 6.3 pIC50 = 6.3 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 457 5 1 5 5.7 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)o1 10.1016/j.bmcl.2009.02.043
118179174 181894 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4786609 181894 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 561 6 1 4 4.6 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
87285732 172383 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4517137 172383 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 630 8 1 8 4.6 Cc1c(N2CCN(Cc3ccc(Cl)nc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
118178989 180572 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4760799 180572 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44444635 154166 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399779 154166 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 637 7 2 4 8.0 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
44402472 132300 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL370145 132300 0 None - 0 Rat 7.3 pIC50 = 7.3 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 619 12 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCCc3ccccn3)c21 10.1016/j.bmcl.2005.03.030
44406776 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.3 pIC50 = 7.3 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
162645007 178881 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44573278 186864 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL493932 186864 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44573277 186863 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL493931 186863 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 498 7 1 5 6.3 CCCn1c(CC)nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44267239 96663 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 413 9 3 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL267558 96663 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 413 9 3 3 5.7 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)nc2)c1 10.1016/s0960-894x(01)00133-0
44293285 162225 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
CHEMBL417189 162225 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of recombinant human Gonadotropin-releasing hormone receptorInhibition of recombinant human Gonadotropin-releasing hormone receptor
ChEMBL 546 7 4 7 6.2 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(NC(=O)Nc4cncnc4)cc3c2OCC[C@@H]2CCCCN2)c1 10.1016/s0960-894x(00)00318-8
44402057 71594 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL197254 71594 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 487 9 2 8 4.8 COCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391693 63436 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL180167 63436 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 605 9 3 5 5.4 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(C(F)(F)F)c(F)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44406776 133819 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24TDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR M24T
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
162645007 178881 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44402672 71291 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 420 7 1 6 5.1 COc1ccc(C#N)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL196351 71291 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 420 7 1 6 5.1 COc1ccc(C#N)cc1CSc1nc2cc(NC(=O)C3CC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44573112 187015 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494739 187015 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 484 7 1 5 5.9 CCCCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
11583388 8206 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092626 8206 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 457 5 2 5 4.8 CCc1nc(CN2CCN(c3cncc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
44346397 114000 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162650892 179649 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4749974 179649 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 554 5 2 6 4.5 N=S1(=O)CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44561141 192897 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL527422 192897 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 432 3 3 4 4.4 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44391498 165567 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL426060 165567 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 524 10 1 7 3.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(OCCN1CCOCC1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
118179127 182632 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
CHEMBL4795998 182632 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 599 7 2 5 4.2 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2CCO 10.1021/acs.jmedchem.0c01076
127036617 137017 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1236 31 17 15 -2.9 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
CHEMBL3754384 137017 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1236 31 17 15 -2.9 CC(C)C[C@H](NC(=O)C1(NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2c[nH]cn2)NC(=O)[C@@H]2CCC(=O)N2)CCCC1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
155531714 175617 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175617 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Antagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against rat GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
44365609 39466 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 11 3 6 5.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(C)(=O)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL147537 39466 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 11 3 6 5.4 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(C)(=O)=O)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
10930638 98572 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44406776 133819 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
3038517 3645 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
CHEMBL22055 3645 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
DB06494 3645 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm060580w
44293366 161662 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL416285 161662 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 511 12 3 3 6.8 CCN(CC)C(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
44293236 174307 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
CHEMBL45639 174307 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 560 13 4 4 5.7 CCNC(=O)c1ccc2[nH]c(-c3cc(C)cc(C)c3)c(CCNCCCCc3ccc(NS(C)(=O)=O)cc3)c2c1 10.1016/s0960-894x(01)00274-8
10674894 25336 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL135103 25336 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL438652 212037 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to monkey anterior pituitary LHRH receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm0512894
10674894 25336 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL135103 25336 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
11980076 206711 27 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL1007 206711 27 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor the membrane fractions of the monkey pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
44321497 97642 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL273390 97642 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.Binding inhibition towards human pituitary gonadotropin-releasing hormone receptor using [125I]buserelin.
ChEMBL 665 11 2 5 7.9 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CCN(C(=O)OC(C)(C)C)CC4)cc3c2[C@H](C)CNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00512-1
CHEMBL436874 211941 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D293E
ChEMBL None None None None 10.1021/jm0506928
11496945 175901 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL459659 175901 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 496 4 3 4 6.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=S)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
145957893 161521 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 545 8 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cc(F)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4160683 161521 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 545 8 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cc(F)cc(F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
11455317 62559 0 None 851 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 62559 0 None 851 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
1185 3645 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44402396 161130 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL413216 161130 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
44402397 161318 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL414899 161318 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
87285768 169927 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4449332 169927 1 None - 0 Human 8.2 pIC50 = 8.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 1 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 739 13 2 9 5.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)o3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44402397 161318 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL414899 161318 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1578 42 17 18 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)C(N)CN)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL3085508 209243 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305K
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL None None None None 10.1021/jm0506928
11180219 110733 0 None 112 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 110733 0 None 112 2 Human 8.2 pIC50 = 8.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptor stimulated calcium fluxInhibition of Human gonadotropin-releasing hormone receptor stimulated calcium flux
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
67142995 169759 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccoc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446997 169759 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 585 8 1 8 4.1 Cc1c(N2CCN(Cc3ccoc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44577104 178169 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1021/jm701249f
CHEMBL468565 178169 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 456 5 2 4 5.4 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1021/jm701249f
11167850 2701 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182A
ChEMBL None None None None 10.1021/jm0506928
11532637 7633 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
CHEMBL1088866 7633 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 0 6 5.1 CCn1cnc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2010.02.099
44406776 133819 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144450 171743 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4475210 171743 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 570 8 1 8 3.5 Cc1c(N2CCN(Cc3ccccc3C#N)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44402396 161130 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
CHEMBL413216 161130 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cellsIn vitro inhibition of human gonadotropin-releasing hormone expressed in HEK293 cells
ChEMBL 1663 44 18 19 1.8 CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(NC(=O)NC(=O)[C@H](N)CCC(N)=O)cc1)C(=O)N[C@H](Cc1ccc(NC(N)=O)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(=O)O 10.1016/j.bmcl.2005.03.085
67143570 171191 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4467407 171191 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 726 14 2 10 5.0 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
71623059 180243 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 180243 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
1184 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
9874838 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
CHEMBL71917 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(01)00779-x
1184 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
9874838 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
CHEMBL71917 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm701249f
9961721 167914 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR D302A mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
9961721 167914 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
10649568 14397 0 None 10 2 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of binding to gonadotropin-releasing hormone receptor in dogIn vitro inhibition of binding to gonadotropin-releasing hormone receptor in dog
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
CHEMBL120432 14397 0 None 10 2 Human 7.2 pIC50 = 7.2 Binding
In vitro inhibition of binding to gonadotropin-releasing hormone receptor in dogIn vitro inhibition of binding to gonadotropin-releasing hormone receptor in dog
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1021/jm000275p
1184 3676 31 None 426 2 Human 7.2 pIC50 = 7.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
9874838 3676 31 None 426 2 Human 7.2 pIC50 = 7.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
CHEMBL71917 3676 31 None 426 2 Human 7.2 pIC50 = 7.2 Binding
Inhibition of Human gonadotropin-releasing hormone receptorInhibition of Human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
1184 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
9874838 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
CHEMBL71917 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)Inhibition of Rat gonadotropin-releasing hormone receptor(moderate affinity)
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm049218c
1184 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
9874838 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
CHEMBL71917 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm0512894
1184 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
9874838 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
CHEMBL71917 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm020180i
1184 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
9874838 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
CHEMBL71917 3676 31 None -426 2 Rat 7.2 pIC50 = 7.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1021/jm9803673
44406776 133819 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL436874 211941 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W291F
ChEMBL None None None None 10.1021/jm0506928
44365078 41213 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 414 10 3 3 5.7 COc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL149062 41213 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 414 10 3 3 5.7 COc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365456 42548 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 11 3 2 7.1 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL150223 42548 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 440 11 3 2 7.1 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
15462666 96055 4 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL262557 96055 4 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cellsDisplacement of [125I]-His5, D-Tyr6]GnRH from GnRHR F272L mutant expressed in COS7 cells
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 141086 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44292915 182309 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 590 12 3 4 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)O)cc3c2CCN(CCCCc2ccc(O)cc2)C(=O)OCc2ccccc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL47921 182309 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 590 12 3 4 8.1 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)O)cc3c2CCN(CCCCc2ccc(O)cc2)C(=O)OCc2ccccc2)c1 10.1016/s0960-894x(01)00274-8
44402378 69333 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL193529 69333 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 457 8 2 7 5.4 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44391612 63168 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL179977 63168 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 471 9 2 6 3.8 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCO)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44365170 40211 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 430 10 3 4 5.3 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
CHEMBL148245 40211 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 430 10 3 4 5.3 COc1ccc(-c2[nH]c3ccccc3c2CCNCCCc2ccc(O)cc2)cc1OC 10.1016/s0960-894x(00)00707-1
44417614 141086 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y284L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
67144531 172582 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(C#N)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4521484 172582 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 8 1 8 4.6 Cc1c(N2CCN(Cc3cccc(C#N)c3F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
162670223 181989 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4787856 181989 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 521 5 2 5 4.6 O=C(Nc1ccc2c(c1)C1(CCC(O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44573790 192659 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
CHEMBL523849 192659 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 5 1 5 5.9 Cc1c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)ncn1C(C)C 10.1016/j.bmcl.2009.02.043
44402464 168523 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL439860 168523 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3ccncc3)c21 10.1016/j.bmcl.2005.03.030
44402404 133041 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL371073 133041 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 568 9 2 8 5.8 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)N3CCCC3)c21 10.1016/j.bmcl.2005.03.030
87285668 173147 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 669 8 1 8 5.6 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4536130 173147 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 669 8 1 8 5.6 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)s3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44444672 168836 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL442283 168836 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 630 8 1 5 6.4 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)C1 10.1016/j.bmcl.2007.09.099
44402538 167871 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL434955 167871 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402538 167871 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL434955 167871 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 471 7 2 7 5.7 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
145954593 161983 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(F)cc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4167945 161983 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 561 8 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3ccc(F)cc3Cl)c2=O)c1F 10.1016/j.ejmech.2017.12.095
44406776 133819 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F313L
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44296134 187814 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCC(C)CN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL50182 187814 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 469 6 2 6 5.9 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2CCC(C)CN2)c1 10.1016/j.bmcl.2003.12.101
44406776 133819 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S118N
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44402232 71067 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL195920 71067 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 454 8 1 7 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)C3CCC3)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44561265 172538 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL452044 172538 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 512 6 3 5 5.0 FC(F)(F)C(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44322336 105660 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 398 6 1 4 5.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC(C)CN(C)C)c1 10.1016/s0960-894x(99)00446-1
CHEMBL313517 105660 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 398 6 1 4 5.5 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCC(C)CN(C)C)c1 10.1016/s0960-894x(99)00446-1
44402462 69562 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 399 6 1 4 5.9 CC(C)n1c(SCc2ccccc2Cl)nc2cc(NC(=O)C3CC3)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL193897 69562 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 399 6 1 4 5.9 CC(C)n1c(SCc2ccccc2Cl)nc2cc(NC(=O)C3CC3)ccc21 10.1016/j.bmcl.2005.03.030
67144164 173314 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
CHEMBL4539811 173314 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 643 9 1 10 3.9 COC(=O)c1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)o1 10.1021/acs.jmedchem.6b01071
44215908 93794 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249982 93794 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 616 7 1 5 6.1 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44444630 154285 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL400390 154285 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
44561108 185848 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL487627 185848 0 None - 0 Rat 4.2 pIC50 = 4.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
71666542 179767 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4751345 179767 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 6 4.4 O=C(NCc1ncc(F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL436874 211941 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL None None None None 10.1021/jm0506928
67143743 170739 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cc1 10.1021/acs.jmedchem.6b01071
CHEMBL4460966 170739 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccc(CN2CCN(c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)cc1 10.1021/acs.jmedchem.6b01071
67144486 170673 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3C(F)(F)F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4459812 170673 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccccc3C(F)(F)F)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
67143407 170201 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4452793 170201 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 613 8 1 7 4.7 Cc1c(N2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44402377 132918 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1cccc(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
CHEMBL370603 132918 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 379 6 1 4 5.6 Cc1cccc(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
44391703 167938 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
CHEMBL435334 167938 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 575 10 3 5 5.2 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1F 10.1016/j.bmcl.2004.10.090
CHEMBL436874 211941 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306K
ChEMBL None None None None 10.1021/jm0506928
162645007 178881 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
44402293 71084 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
CHEMBL196040 71084 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 520 8 2 8 5.6 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1Cc1ccccn1 10.1016/j.bmcl.2005.03.030
44391526 122091 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL360244 122091 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 560 12 2 6 5.6 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCCNCc1ccccc1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
86272223 115688 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
CHEMBL3358415 115688 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 737 7 1 7 6.0 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1cccc(OC(F)(F)F)c1 10.1021/ml5004469
118179235 181353 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4779806 181353 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 548 5 1 5 4.3 CC(=O)N1CCC2(CC1)c1cc(NC(=O)c3cccnc3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
44573714 187103 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 2 4 5.2 Cc1n[nH]c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL495189 187103 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 2 4 5.2 Cc1n[nH]c(C)c1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44561368 176240 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 176240 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44573275 186832 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493730 186832 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 470 6 1 5 5.6 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1CC 10.1016/j.bmcl.2009.02.043
44402465 134712 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
CHEMBL372455 134712 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 605 11 3 9 5.9 CCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)cc(C(=O)NCc3cccnc3)c21 10.1016/j.bmcl.2005.03.030
145949379 162164 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 496 7 1 7 3.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccnc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4170863 162164 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 496 7 1 7 3.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccnc3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL3085508 209243 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44391734 122103 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL360297 122103 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 509 10 3 5 3.6 CCNC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44391692 63969 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181057 63969 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 437 7 1 4 4.8 CC(C)c1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44444644 154460 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401350 154460 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 601 6 1 4 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(C(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44365844 41686 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 12 3 6 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(=O)(=O)C(C)C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL149447 41686 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Binding affinity to rat Gonadotropin-releasing hormone receptor.Binding affinity to rat Gonadotropin-releasing hormone receptor.
ChEMBL 646 12 3 6 6.2 Cc1cc(C)cc(-c2[nH]c3ccc(OC(=O)N4CCN(S(=O)(=O)C(C)C)CC4)cc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00708-3
CHEMBL97265 214146 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)NCC(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
24825725 192027 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
CHEMBL521674 192027 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 456 5 1 5 5.4 CCn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1C 10.1016/j.bmcl.2009.02.043
44305274 102296 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 667 11 1 9 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccsc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
CHEMBL305155 102296 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cellsIn vitro inhibition of specific [125I]leuprorelin binding to the cloned human LHRH receptor expressed in chinese hamster ovary cells
ChEMBL 667 11 1 9 6.6 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)c4ccsc4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00372-4
44293222 175387 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL138464 175387 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
CHEMBL45883 175387 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 531 7 3 7 5.8 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c(C(=O)Nc4cnccn4)cc3c2OCCC2CCCCN2)c1 10.1016/s0960-894x(00)00024-x
11525358 186759 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmc.2012.09.013
CHEMBL493185 186759 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmc.2012.09.013
10074296 9298 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL11149 9298 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)Inhibition of [125I]buserelin binding to rat pituitary Gonadotropin-releasing hormone receptor, in the absence of bovine serum albumin (BSA)
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00274-8
CHEMBL438652 212037 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptorInhibition of [125I]leuprorelin binding to rat anterior pituitary LHRH receptor
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cc2ccccc2[nH]1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(N)=O 10.1021/jm0512894
10074296 9298 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
CHEMBL11149 9298 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat GnRH receptor bindingInhibition of rat GnRH receptor binding
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00134-2
10074296 9298 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11149 9298 0 None - 0 Rat 8.2 pIC50 = 8.2 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00133-0
10074296 9298 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
CHEMBL11149 9298 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligandInhibitory activity against human GnRH receptor using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt]GnRH radioligand
ChEMBL 489 11 3 3 6.0 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(NS(C)(=O)=O)cc2)c1 10.1016/s0960-894x(01)00779-x
11980076 206711 27 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
CHEMBL1007 206711 27 None - 1 Rat 8.2 pIC50 = 8.2 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm9803673
67144646 172566 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3cocn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4521118 172566 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 586 8 1 9 3.5 Cc1c(N2CCN(Cc3cocn3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
155559612 174311 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1612 43 20 24 -4.1 CC(C)C[C@H](NC(=O)[C@H](CCCCNC(=O)CCCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
CHEMBL4563936 174311 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Displacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting methodDisplacement of [125I]-D-Tyr6-His5-GnRH from recombinant human GnRH receptor expressed in HEK293 cell membrane measured after 16 to 19 hrs by gamma counting method
ChEMBL 1612 43 20 24 -4.1 CC(C)C[C@H](NC(=O)[C@H](CCCCNC(=O)CCCC(=O)OC[C@H]1O[C@@H](n2ccc(N)nc2=O)C(F)(F)[C@@H]1O)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)C1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2019.01.041
44292918 170849 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
CHEMBL44627 170849 0 None - 0 Human 8.2 pIC50 = 8.2 Binding
Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to human Gonadotropin-releasing hormone receptor.
ChEMBL 552 14 2 3 7.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(=O)N(CC(C)C)CC(C)C)cc3c2CCNCCCCc2ccncc2)c1 10.1016/s0960-894x(01)00275-x
67143413 169050 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL4436711 169050 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 610 8 1 8 4.3 Cc1cncc(CN2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)CC2)c1 10.1021/acs.jmedchem.6b01071
CHEMBL3085508 209243 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q189E
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
70691201 77300 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
CHEMBL2088506 77300 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human prostate cancer membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
11604354 186941 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
CHEMBL494400 186941 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 2 4 4.9 Cc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c[nH]1 10.1016/j.bmcl.2009.02.043
11167850 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
145952802 162047 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 579 8 1 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccc(OC(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4169027 162047 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 579 8 1 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3cccc(OC(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL3085508 209243 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302NDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR D302N
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H182E
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
CHEMBL94842 214135 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44417614 141086 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Q208E mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417614 141086 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10722009 116053 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL336319 116053 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
44295982 187716 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2Cc3ccccc3CN2)c1 10.1016/j.bmcl.2003.12.101
CHEMBL50035 187716 0 None - 0 Rat 7.2 pIC50 = 7.2 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.3 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@@H]2Cc3ccccc3CN2)c1 10.1016/j.bmcl.2003.12.101
10722009 116053 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL336319 116053 0 None - 0 Human 7.2 pIC50 = 7.2 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
ChEMBL 582 11 0 8 6.6 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
44365281 42552 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1cc(OC)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL150228 42552 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 444 11 3 4 5.7 COc1cc(OC)cc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
15462665 168094 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 615 9 0 7 7.4 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(C2CCCCC2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL436346 168094 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 615 9 0 7 7.4 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(C2CCCCC2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44412876 77557 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccccc3OC)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL209419 77557 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 552 10 0 7 6.6 CCOC(=O)c1cn(Cc2ccccc2)c2sc(-c3ccccc3OC)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10985312 78336 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 78336 0 None - 1 Rat 6.2 pIC50 = 6.2 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitariesTested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in rat anterior pituitaries
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
44322390 204884 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 3 1 4 5.1 CN1CCCCC(Oc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
CHEMBL89041 204884 0 None - 0 Rat 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 3 1 4 5.1 CN1CCCCC(Oc2c(-c3ccccc3)c(O)nc3cc(Cl)ccc23)C1 10.1016/s0960-894x(99)00446-1
11512807 139606 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 610 11 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(Cc3ccccc3)C(C)=O)c2c1=O 10.1021/jm0512894
CHEMBL380200 139606 0 None - 0 Human 5.2 pIC50 = 5.2 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 610 11 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2OC)c2sc(-c3ccc(OC)cc3)c(CN(Cc3ccccc3)C(C)=O)c2c1=O 10.1021/jm0512894
44573507 186971 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 4 5.8 Cc1ccc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494548 186971 0 None - 0 Human 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 428 4 1 4 5.8 Cc1ccc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
11496610 4012 11 None - 2 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
5582 4012 11 None - 2 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
CHEMBL474991 4012 11 None - 2 Rat 7.2 pIC50 = 7.2 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1021/jm801572m
25193798 169631 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL444509 169631 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 562 6 2 5 6.6 CC(C)(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
10919052 113020 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113020 0 None - 1 Human 6.2 pIC50 = 6.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306A mutant expressed in COS7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44402038 69864 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL194074 69864 0 None - 0 Rat 6.2 pIC50 = 6.2 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44346398 14369 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL120260 14369 0 None - 1 Human 5.2 pIC50 = 5.2 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
162675445 182826 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4798298 182826 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 470 6 1 4 4.4 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3CC2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL2370256 208075 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm990433g
44561369 189874 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL517881 189874 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 508 4 3 5 4.4 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
11496610 4012 11 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
5582 4012 11 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
CHEMBL474991 4012 11 None - 2 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 1 5 5.8 CC(c1ccc(cc1)c1[nH]c2c(n1)cccc2N1CCN(CC1)Cc1ccc2c(c1)nccn2)(C)C 10.1016/j.bmcl.2010.02.099
44391613 167712 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
CHEMBL433954 167712 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 462 9 1 7 2.4 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1CCN1CCOCC1 10.1016/j.bmcl.2004.10.089
127036774 136984 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1146 25 12 13 -1.5 CC(C)C[C@H](NC(=O)CN1CN(c2ccccc2)C2(CCN(C(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@@H]3CCC(=O)N3)CC2)C1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
CHEMBL3754120 136984 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysisDisplacement of [125I]-DTyr6-His5-GnRH from human type 1 GnRH receptor expressed in HEK293 cell membranes after 16 to 19 hrs by gamma counting analysis
ChEMBL 1146 25 12 13 -1.5 CC(C)C[C@H](NC(=O)CN1CN(c2ccccc2)C2(CCN(C(=O)[C@H](Cc3c[nH]c4ccccc34)NC(=O)[C@H](Cc3c[nH]cn3)NC(=O)[C@@H]3CCC(=O)N3)CC2)C1=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1039/C5MD00259A
162645007 178881 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
145949556 162383 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4174298 162383 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 485 7 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccco3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
67142794 173551 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
CHEMBL4545859 173551 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 559 8 1 7 4.0 Cc1ccccc1CN1CCN(c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)CC1 10.1021/acs.jmedchem.6b01071
162645007 178881 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4740709 178881 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Antagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at rat GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 498 6 1 4 5.2 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C(C)(C)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL428619 211713 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44444649 154466 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401418 154466 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 646 10 3 7 4.4 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(O)CN3CCNCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44185958 154459 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL401349 154459 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 615 8 1 5 5.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCN(CC(=O)N3CCCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
44573586 186918 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
CHEMBL494232 186918 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 443 4 1 5 5.5 Cc1nc(C)c(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)o1 10.1016/j.bmcl.2009.02.043
44391821 65250 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183197 65250 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 538 9 2 6 4.8 CC(C)(C)OC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
67143567 170703 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCC(C)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4460413 170703 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCC(C)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44295833 167347 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCc3ccccc32)c1 10.1016/j.bmcl.2003.12.101
CHEMBL431344 167347 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelinInhibitory concentration against binding of rat Gonadotropin-releasing hormone receptor using [125I]buserelin
ChEMBL 503 6 2 6 6.4 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCCC2NCCc3ccccc32)c1 10.1016/j.bmcl.2003.12.101
11318649 64023 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL181257 64023 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 537 9 3 5 4.3 CC(C)(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccccc3F)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44322434 110928 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 6 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCCN2CCCCC2)c1 10.1016/s0960-894x(99)00446-1
CHEMBL327323 110928 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 424 6 1 4 6.1 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)ccc3c2OCCCN2CCCCC2)c1 10.1016/s0960-894x(99)00446-1
44444673 93847 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
CHEMBL250389 93847 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 644 8 1 5 6.8 COC1CCN(C(=O)C2CCN(CCc3c(-c4cc(C)cc(C)c4)[nH]c4sc(C(C)(C)C(=O)N5C6CCC5CC6)cc34)CC2)CC1 10.1016/j.bmcl.2007.09.099
118179169 179346 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4746174 179346 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 613 6 1 4 5.4 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccc(F)cc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
162656174 180292 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
CHEMBL4757424 180292 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 589 5 2 5 5.6 O=C(Nc1ccc2c(c1)C1(CCC(O)(C(F)(F)F)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1)c1cccnc1 10.1021/acs.jmedchem.0c01076
44573111 187014 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494738 187014 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 456 5 1 5 5.1 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)cn1C 10.1016/j.bmcl.2009.02.043
44444628 93883 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL250568 93883 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 722 8 2 5 8.8 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2[C@H](C)CN/C(=N/C(=O)OC(C)C)N2CCC(c3ccncc3)CC2)c1 10.1016/j.bmcl.2007.09.099
44402616 70792 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
CHEMBL195516 70792 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
44391718 65274 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL183325 65274 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 523 10 3 5 4.0 CC(C)NC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
44593415 188790 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL512893 188790 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
44573276 186833 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
CHEMBL493731 186833 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 484 6 1 5 5.9 CCc1nc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)n1CC 10.1016/j.bmcl.2009.02.043
11167850 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203PDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S203P
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44444626 154344 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
CHEMBL400739 154344 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 680 7 2 5 7.6 COC(=O)/N=C(/NC[C@@H](C)c1c(-c2cc(C)cc(C)c2)[nH]c2sc(C(C)(C)C(=O)N3C4CCC3CC4)cc12)N1CCC(c2ccncc2)C1 10.1016/j.bmcl.2007.09.099
11592658 79341 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 642 11 2 6 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)NC(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL211731 79341 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 642 11 2 6 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)c(C(=O)NC(C)C)cn3Cc2c(F)cccc2F)cc1 10.1021/jm0512894
CHEMBL436874 211941 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHRDisplacement of [125I]-His5, D-Tyr6]GnRH from human wild type GnRHR
ChEMBL None None None None 10.1021/jm0506928
44341186 9949 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL115192 9949 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Concentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptorConcentration required for the inhibition of I-125 labeled buserelin binding to the human Gonadotropin-releasing hormone receptor
ChEMBL 606 10 3 4 7.2 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4CC5CCC4CC5)cc3c2[C@H](C)CNCCc2ccnc(C(=O)O)c2)c1 10.1016/s0960-894x(02)00751-5
CHEMBL436874 211941 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K115Q
ChEMBL None None None None 10.1021/jm0506928
44293378 101423 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
CHEMBL300792 101423 0 None - 0 Rat 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.Inhibition of [125I]buserelin binding to rat Gonadotropin-releasing hormone receptor.
ChEMBL 618 13 1 3 8.8 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN(CCCCc2ccncc2)CC(C)C)c1 10.1016/s0960-894x(01)00275-x
1185 3645 32 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280FDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR W280F
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44561368 176240 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL460892 176240 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 480 4 3 4 5.0 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5cccc6[nH]c(=O)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
44406776 133819 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N27A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
11167850 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300VDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300V
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR S168A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
67144496 169267 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4439817 169267 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44274248 98220 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2Cl)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL277435 98220 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.Antagonist concentration required to inhibit specific binding of [125I]leuprorelin to human luteinizing releasing hormone receptor in cloned chinese hamster ovary (CHO) cells.
ChEMBL 643 9 0 7 7.5 COc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2Cl)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
11167850 2701 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300K
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
67143514 172829 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCCC(C)C2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL4528231 172829 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 468 6 1 6 3.6 Cc1c(N2CCCC(C)C2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
44593415 188790 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1021/jm701249f
CHEMBL512893 188790 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Binding affinity at human GnRH receptor by competition binding assayBinding affinity at human GnRH receptor by competition binding assay
ChEMBL 462 5 3 5 4.3 FC(F)(F)c1nc2c(N3CCN(CCOc4cccc5[nH]c(=S)[nH]c45)CC3)cccc2[nH]1 10.1021/jm701249f
10930638 98572 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL280212 98572 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 698 10 1 7 8.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)c3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44417615 141391 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL387006 141391 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR H306E mutant expressed in COS7 cells
ChEMBL 662 9 2 9 6.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC3=NCCN3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
10674894 25336 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL135103 25336 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
ChEMBL 588 10 0 7 6.9 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm9803673
CHEMBL261927 208776 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1ccccn1)C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
15602807 8136 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1092245 8136 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 476 4 0 6 5.6 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5ccc6nccnc6c5)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
44391628 65541 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL183572 65541 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 513 10 1 7 4.4 CCOC(=O)CSc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44406776 133819 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
44391542 64896 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182639 64896 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
44573753 186888 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
CHEMBL494021 186888 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 442 4 1 5 4.9 Cc1cc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)nn1C 10.1016/j.bmcl.2009.02.043
44391735 121823 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
CHEMBL359914 121823 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 591 10 3 5 5.7 O=C(NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1)Nc1ccccc1Cl 10.1016/j.bmcl.2004.10.090
44391771 165469 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL425524 165469 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 551 10 3 5 4.7 CC(C)(C)NC(=O)NCCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
86275343 182909 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4799511 182909 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 655 6 1 6 4.7 O=C(NCc1ncc(C(F)(F)F)cc1F)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
44391835 165751 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
CHEMBL427146 165751 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 536 10 2 5 4.8 CC(C)(C)CC(=O)NCCc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.090
15895696 111972 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
CHEMBL329834 111972 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Binding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligandBinding affinity for Gonadotropin-releasing hormone receptor in rat pituitary membrane at 10 buserelin as radioligand
ChEMBL 469 6 1 6 6.0 Cc1cc(C)cc(-c2c(O)nc3cc(Cl)c([N+](=O)[O-])cc3c2OCC[C@H]2CCCCN2C)c1 10.1016/s0960-894x(99)00447-3
44573585 186657 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL492587 186657 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
67143612 170483 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4456937 170483 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 638 9 2 8 3.6 Cc1c(N2CCN(Cc3cccc(C(N)=O)c3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
44359289 12045 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL1184180 12045 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
CHEMBL337323 12045 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 547 8 3 7 6.3 CCn1nccc1NC(=O)c1cc2c(OCCC3CCCCN3)c(-c3cc(C)cc(C)c3)c(O)nc2cc1Cl 10.1016/s0960-894x(00)00024-x
44402616 70792 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
CHEMBL195516 70792 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 469 7 2 7 5.5 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)NC(C)(C)C)ccc2n1C1CC1 10.1016/j.bmcl.2005.03.030
11167850 2701 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1178 2701 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
1187 2701 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
CHEMBL179691 2701 22 None 6309 2 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/acs.jmedchem.6b01071
118179135 181436 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4780737 181436 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
44572286 180219 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
CHEMBL475650 180219 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Displacement of [D-Trp6]-GnRH from rat recombinant GnRH receptorDisplacement of [D-Trp6]-GnRH from rat recombinant GnRH receptor
ChEMBL 494 4 3 5 5.2 CC(C)(C)c1ccc(-c2nc3c(N4CCN(Cc5ccc6c(c5)NCC(=O)N6)CC4)cccc3[nH]2)cc1 10.1021/jm801572m
44406776 133819 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR L300A
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL2370262 208078 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Concentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranesConcentration of the peptide which displaces 50% of 125 I-[D-Lys6] gonadotropin-releasing hormone bound to rat pituitary membranes
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H](C)NC(=O)[C@@H](Cc1ccccn1)NC(=O)[C@@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm990433g
44444675 154184 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL399857 154184 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 630 7 1 5 6.3 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(C(=O)N3CCOCC3)C(C)C2)c1 10.1016/j.bmcl.2007.09.099
44402038 69864 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
CHEMBL194074 69864 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 472 7 1 8 6.2 COc1ccc([N+](=O)[O-])cc1CSc1nc2cc(NC(=O)OC(C)(C)C)ccc2n1C(C)C 10.1016/j.bmcl.2005.03.030
44402673 132747 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
CHEMBL370414 132747 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Inhibitory concentration against rat leutinizing releasing hormone receptorInhibitory concentration against rat leutinizing releasing hormone receptor
ChEMBL 499 10 2 7 6.4 CCCCCn1c(SCc2cc([N+](=O)[O-])ccc2OC)nc2cc(NC(=O)NC(C)(C)C)ccc21 10.1016/j.bmcl.2005.03.030
44391670 64361 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
CHEMBL181864 64361 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Inhibitory concentration towards human leutinizing releasing hormone receptorInhibitory concentration towards human leutinizing releasing hormone receptor
ChEMBL 473 8 1 5 4.8 CCOc1nc2cc(S(=O)(=O)NCc3ccc(F)cc3)ccc2n1Cc1cccc(Cl)c1 10.1016/j.bmcl.2004.10.089
67143618 169727 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4446435 169727 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 637 8 1 10 4.1 Cc1c(N2CCN(Cc3cccc4nonc34)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
67143023 174425 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4566719 174425 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 656 9 2 10 4.2 Cc1c(N2CCN(Cc3cccc([N+](=O)[O-])c3)CC2)c(=O)n(C[C@H](N)c2ccccc2O)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
155531714 175617 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
CHEMBL4593521 175617 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Displacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assayDisplacement of [125I]D-Trp6-LHRH from rat GnRH receptor expressed in HEK293 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL 715 13 2 9 5.2 COc1cccc(N2CCN(c3c(C)n(Cc4c(F)cccc4C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c4ccccc4)c3=O)CC2)c1F 10.1021/acs.jmedchem.6b01071
145949399 162184 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 8 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(C(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
CHEMBL4171288 162184 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting methodDisplacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cells after 1 hr by microbeta scintillation counting method
ChEMBL 577 8 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(N)Cc3cccc(C(F)(F)F)c3)c2=O)c1F 10.1016/j.ejmech.2017.12.095
9961721 167914 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
CHEMBL435167 167914 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm060580w
44359254 11527 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL1180716 11527 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
CHEMBL139292 11527 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
In vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptorIn vitro inhibitory activity against rat CHO cells stably expressing human gonadotropin-releasing hormone receptor
ChEMBL 561 8 3 8 5.8 COc1nccc(NC(=O)c2cc3c(OCCC4CCCCN4)c(-c4cc(C)cc(C)c4)c(O)nc3cc2Cl)n1 10.1016/s0960-894x(00)00024-x
11549071 138417 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 11 2 7 6.4 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CN)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
CHEMBL378481 138417 0 None - 0 Human 8.1 pIC50 = 8.1 Binding
Inhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cellsInhibition of [125I]leuprorelin binding to human recombinant LHRH receptor expressed in CHO cells
ChEMBL 628 11 2 7 6.4 CC(C)C(=O)c1cn(Cc2c(F)cccc2F)c2sc(-c3ccc(NC(=O)CN)cc3)c(CN(C)Cc3ccccc3)c2c1=O 10.1021/jm0512894
10985312 78336 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
CHEMBL21126 78336 0 None - 1 Human 8.1 pIC50 = 8.1 Binding
Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)Tested for antagonist concentration required to inhibit specific binding of [125I]leuprorelin to Leutinizing releasing hormone receptor in monkey (chinese hamster ovary (CHO) cells)
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1021/jm020180i
70691201 77300 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
CHEMBL2088506 77300 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma countingDisplacement of [125I][D-Trp6]GnRH1 from GnRH receptor expressed in human pituitary membrane by gamma counting
ChEMBL 1952 47 22 28 -0.7 CCCC(=O)NCCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCCNC(=O)CO/N=C(\C)[C@]1(O)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](N)[C@H](O)[C@H](C)O2)C1)C(=O)c1c(OC)cccc1C3=O)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1016/j.ejmech.2012.08.014
11167850 2701 22 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208E
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44348333 96445 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL265727 96445 0 None - 0 Rat 8.0 pIC50 = 8.0 Binding
Inhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranesInhibition of binding of radiolabeled histrelin to Gonadotropin-releasing hormone receptor (GnRHr) in rat pituitary gland membranes
ChEMBL 1575 40 14 17 2.9 CC(=O)Nc1ccc(C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](NC(C)=O)N(C)C(=O)c2ccc3ccccc3c2)C(=O)N[C@H](Cc2ccc(NC(C)=O)cc2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)cc1 10.1021/jm970024p
CHEMBL3085508 209243 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR N305D
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
44406776 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL371722 133819 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295KDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR E295K
ChEMBL 609 14 2 3 8.8 COc1c(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N(CC(C)C)CC(C)C)cc3c2[C@H](C)CNCCc2ccccc2)cc1C 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR F309Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
1185 3645 32 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208DDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Q208D
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL3085508 209243 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290QDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290Q
ChEMBL None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H]1NCCC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm0506928
15602806 8212 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
CHEMBL1092638 8212 0 None - 0 Human 8.0 pIC50 = 8.0 Binding
Displacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from human recombinant GNRH receptor by scintillation counting
ChEMBL 456 5 1 5 5.2 CCc1nc(CN2CCN(c3cccn4cc(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c(C)[nH]1 10.1016/j.bmcl.2010.02.099
71623059 180243 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4756920 180243 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 603 6 1 6 4.2 O=C(NCc1ncccc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
118179135 181436 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
CHEMBL4780737 181436 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 5 1 4 4.9 CC(=O)N1CCC2(CC1)c1cc(C(=O)NCc3ccccc3Cl)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C 10.1021/acs.jmedchem.0c01076
44573585 186657 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
CHEMBL492587 186657 0 None - 0 Human 7.1 pIC50 = 7.1 Binding
Displacement of [125I]-(D-Trp6)-GnRH from human GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from human GnRH receptor
ChEMBL 429 4 1 5 5.1 Cc1ncoc1CN1CCN(c2cccc3[nH]c(-c4ccc(C(C)(C)C)cc4)nc23)CC1 10.1016/j.bmcl.2009.02.043
44267240 9604 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 427 10 2 3 6.0 COc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
CHEMBL11310 9604 0 None - 0 Rat 7.1 pIC50 = 7.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 427 10 2 3 6.0 COc1ccc(CCCCNCCc2c(-c3cc(C)cc(C)c3)[nH]c3ccccc23)cn1 10.1016/s0960-894x(01)00133-0
44365088 120981 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 10 3 2 6.3 CCc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL358260 120981 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 10 3 2 6.3 CCc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44365500 164731 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1C 10.1016/s0960-894x(00)00707-1
CHEMBL423215 164731 0 None - 0 Rat 6.1 pIC50 = 6.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 412 9 3 2 6.3 Cc1cccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)c1C 10.1016/s0960-894x(00)00707-1
44417614 141086 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL385175 141086 0 None - 0 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 727 11 2 7 8.2 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCc3ccccc3)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44346397 114000 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL333518 114000 0 None - 1 Human 6.1 pIC50 = 6.1 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR Y290L mutant expressed in COS7 cells
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44365374 41414 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1 10.1016/s0960-894x(00)00707-1
CHEMBL149196 41414 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 398 9 3 2 6.0 Cc1ccc(-c2[nH]c3ccccc3c2CCNCCCCc2ccc(O)cc2)cc1 10.1016/s0960-894x(00)00707-1
44365249 120563 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 370 6 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
CHEMBL357025 120563 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Ability to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptorAbility to displace [125I]- - radio-labeled buserelin from rat Gonadotropin-releasing hormone receptor
ChEMBL 370 6 3 2 5.5 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccc(O)cc2)c1 10.1016/s0960-894x(00)00707-1
44322272 204458 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.1 CN1CCCCC1COc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
CHEMBL86365 204458 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 382 4 1 4 5.1 CN1CCCCC1COc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
44322052 204969 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 356 6 1 4 4.6 CN(C)CCCOc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
CHEMBL89675 204969 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.Inhibition of [125I]buserelin to GnRH receptor in rat pituitary membranes.
ChEMBL 356 6 1 4 4.6 CN(C)CCCOc1c(-c2ccccc2)c(O)nc2cc(Cl)ccc12 10.1016/s0960-894x(99)00446-1
44267257 9273 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
CHEMBL11134 9273 0 None - 0 Rat 5.1 pIC50 = 5.1 Binding
Inhibition of rat gonadotropin-releasing hormone receptorInhibition of rat gonadotropin-releasing hormone receptor
ChEMBL 355 6 2 2 5.2 Cc1cc(C)cc(-c2[nH]c3ccccc3c2CCNCc2ccncc2)c1 10.1016/s0960-894x(01)00133-0
118178989 180572 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
CHEMBL4760799 180572 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 621 6 1 4 5.8 CC(=O)N1CCC2(CC1)c1cc(C(=O)NC3(c4ccc(Cl)cc4)CC3)ccc1N(S(=O)(=O)c1ccc(F)cc1)C2C1CC1 10.1021/acs.jmedchem.0c01076
71666685 182132 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4789613 182132 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 569 6 1 6 3.6 O=C(NCc1ccccn1)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(F)cc1 10.1021/acs.jmedchem.0c01076
67144496 169267 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
CHEMBL4439817 169267 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Antagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assayAntagonist activity against human GnRH receptor expressed in HEK293 cells co-transfected with pGL4-NFAT promoter AP1-luc assessed as inhibition of 20 nM GnRH-induced NFAT activation pre-incubated for 1 hr before GnRH stimulation and measured after 6 hrs by luciferase reporter gene assay
ChEMBL 602 8 1 9 4.0 Cc1c(N2CCN(Cc3cncs3)CC2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.6b01071
86275573 115689 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
CHEMBL3358416 115689 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Antagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assayAntagonist activity against human GnRH receptor expressed in CHO cells by IP-one HTRF assay
ChEMBL 687 6 1 6 5.8 O=C(NCc1ncc(C(F)(F)F)cc1Cl)c1ccc2c(c1)C1(CCS(=O)(=O)CC1)C(C1CC1)N2S(=O)(=O)c1ccc(Cl)cc1 10.1021/ml5004469
44444663 93766 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL249771 93766 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from rat GnRH receptorDisplacement of [125I]D-Trp from rat GnRH receptor
ChEMBL 645 8 2 5 6.2 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2CCN2CCC(CNC(=O)N3CCOCC3)CC2)c1 10.1016/j.bmcl.2007.09.099
1185 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
3038517 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
CHEMBL22055 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
DB06494 3645 32 None - 1 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306EDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR H306E
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1021/jm0506928
44391525 165813 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL427500 165813 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 467 9 1 6 4.7 CCSc1nc2cc(S(=O)(=O)NCc3ccc(OC)cc3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2004.10.089
15602804 7998 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
CHEMBL1091209 7998 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation countingDisplacement of [125I]D-Trp6-GnRH from rat recombinant GNRH receptor by scintillation counting
ChEMBL 458 4 2 6 3.0 CC(C)(C)c1ccc(-c2cn3cccc(N4CCN(Cc5c[nH]c(=O)[nH]c5=O)CC4)c3n2)cc1 10.1016/j.bmcl.2010.02.099
10919052 113020 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
CHEMBL332138 113020 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Displacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cellsDisplacement of [His5, D-Tyr6]GnRH from GnRHR F309L mutant expressed in COS-7 cells
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1021/jm060580w
44561108 185848 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL487627 185848 0 None - 0 Human 5.0 pIC50 = 5.0 Binding
Displacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from human recombinant GnRH receptor
ChEMBL 468 3 2 4 4.8 FC(F)(F)c1nc2c(N3CCN(Cc4cccc5nc(C(F)(F)F)[nH]c45)CC3)cccc2[nH]1 10.1016/j.bmc.2008.05.024
CHEMBL436874 211941 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290LDisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR Y290L
ChEMBL None None None None 10.1021/jm0506928
44444630 154285 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
CHEMBL400390 154285 0 None - 0 Human 7.0 pIC50 = 7.0 Binding
Displacement of [125I]D-Trp from human GnRH receptor expressed in HEK cellsDisplacement of [125I]D-Trp from human GnRH receptor expressed in HEK cells
ChEMBL 596 7 2 3 7.7 Cc1cc(C)cc(-c2[nH]c3sc(C(C)(C)C(=O)N4CCCC4)cc3c2[C@H](C)CNC(=O)N2CCC(c3ccccc3)C2)c1 10.1016/j.bmcl.2007.09.099
44391542 64896 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
CHEMBL182639 64896 0 None - 0 Rat 6.0 pIC50 = 6.0 Binding
Inhibitory concentration towards rat leutinizing releasing hormone receptorInhibitory concentration towards rat leutinizing releasing hormone receptor
ChEMBL 518 9 1 6 5.4 O=S(=O)(NCc1ccc(F)cc1)c1ccc2c(c1)nc(SCc1ccccn1)n2Cc1ccccc1 10.1016/j.bmcl.2004.10.089
11626096 186687 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
CHEMBL492780 186687 0 None - 0 Rat 7.0 pIC50 = 7.0 Binding
Displacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptorDisplacement of [125I]-(D-Trp6)-GnRH from rat GnRH receptor
ChEMBL 428 4 1 5 4.6 Cn1cnc(CN2CCN(c3cccc4[nH]c(-c5ccc(C(C)(C)C)cc5)nc34)CC2)c1 10.1016/j.bmcl.2009.02.043
11167850 2701 22 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1178 2701 22 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
1187 2701 22 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
CHEMBL179691 2701 22 None 6309 2 Human 6.0 pIC50 = 6.0 Binding
Displacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121ADisplacement of [125I]-His5, D-Tyr6]GnRH from mutant GnRHR, GnRHR K121A
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm0506928
44402648 70953 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 453 8 1 7 5.1 COC(=O)c1ccc(OC)c(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
CHEMBL195726 70953 0 None - 0 Human 6.0 pIC50 = 6.0 Binding
Inhibitory concentration against human leutinizing releasing hormone receptorInhibitory concentration against human leutinizing releasing hormone receptor
ChEMBL 453 8 1 7 5.1 COC(=O)c1ccc(OC)c(CSc2nc3cc(NC(=O)C4CC4)ccc3n2C(C)C)c1 10.1016/j.bmcl.2005.03.030
118167818 178852 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
CHEMBL4740373 178852 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of LHRH-induced response preincubated for 20 mins followed by LHRH addition and measured after 60 mins by TR-FRET assay
ChEMBL 527 5 2 4 4.6 CC1N(S(=O)(=O)c2ccc(F)cc2)c2ccc(C(=O)NCc3ccccc3Cl)cc2C12CCNCC2 10.1021/acs.jmedchem.0c01076
118179051 179638 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
CHEMBL4749790 179638 0 None - 0 Human 7.0 pIC50 = 7 Binding
Antagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assayAntagonist activity at human GnRH receptor expressed in CHO-K1 cells assessed as inhibition of buserelin-induced response preincubated for 20 mins followed by buserelin addition and measured after 60 mins by TR-FRET assay
ChEMBL 581 6 1 5 4.8 COc1ccc(S(=O)(=O)N2c3ccc(C(=O)NCc4ccccc4Cl)cc3C3(CCN(C(C)=O)CC3)C2C)cc1 10.1021/acs.jmedchem.0c01076
25193797 189073 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL515200 189073 0 None - 0 Rat 6.0 pIC50 = 6 Binding
Displacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptorDisplacement of [125I]-(D-Trp6)LHRH from rat recombinant GnRH receptor
ChEMBL 548 7 2 5 6.4 CC(C)c1ccc(-c2nc3c(N4CCN(CCOc5cccc6nc(C(F)(F)F)[nH]c56)CC4)cccc3[nH]2)cc1 10.1016/j.bmc.2008.05.024
CHEMBL414113 211362 0 None - 1 Rat 10.1 pKd = 10.1 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
101609491 141284 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
44317046 141284 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
77058850 141284 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
CHEMBL386314 141284 0 None - 1 Rat 10.0 pKd = 10.0 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1555 45 18 19 -1.1 CCCC/N=C(/NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O)NC(N)=O 10.1021/jm00112a013
1190 869 41 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
25074887 869 41 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
583 869 41 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
CHEMBL1200490 869 41 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
DB00050 869 41 None - 1 Human 9.9 pKd = 9.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01076
CHEMBL2369860 207967 0 None - 1 Rat 9.7 pKd = 9.7 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCNc1n[nH]c(N)n1)NC(=O)[C@H](CCCNc1n[nH]c(N)n1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2370807 208178 0 None - 1 Human 9.7 pKd = 9.7 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
3823 49951 38 None -1 11 Rat 9.7 pKd = 9.7 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 49951 38 None -1 11 Rat 9.7 pKd = 9.7 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 49951 38 None -1 11 Rat 9.7 pKd = 9.7 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL414391 211382 0 None - 1 Rat 9.6 pKd = 9.6 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None C/N=C(\NC#N)NCCCC[C@@H](NC(=O)[C@H](CCCCN/C(=N\C)NC#N)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL407225 210902 0 None - 1 Rat 9.6 pKd = 9.6 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(N)=O)c1cccnc1)c1cccnc1 10.1021/jm00398a030
CHEMBL266716 208949 0 None - 1 Human 9.6 pKd = 9.6 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
CHEMBL218396 207650 0 None - 1 Rat 9.6 pKd = 9.6 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL269583 209053 0 None - 1 Rat 9.6 pKd = 9.6 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CCCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL376017 210493 0 None - 1 Rat 9.6 pKd = 9.6 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CC=C[C@H]1C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(=O)O 10.1021/jm00398a030
CHEMBL438762 212047 0 None - 1 Rat 9.5 pKd = 9.5 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCC/N=C(/NC#N)NC(C)C)NC(=O)[C@H](CCCC/N=C(/NC#N)NC(C)C)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2370809 208180 0 None - 1 Human 9.5 pKd = 9.5 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCNC(=O)c1cccnc1)C(=O)N[C@@H](CCCCNC(=O)c1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
10348973 3261 50 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5432 3261 50 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5586 3261 50 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
CHEMBL1800159 3261 50 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
DB11853 3261 50 None - 1 Human 9.4 pKd = 9.4 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
3823 49951 38 None -1 11 Rat 9.4 pKd = 9.4 Binding
Dissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 49951 38 None -1 11 Rat 9.4 pKd = 9.4 Binding
Dissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 49951 38 None -1 11 Rat 9.4 pKd = 9.4 Binding
Dissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes, at concentration 1.0*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL261999 208780 0 None - 1 Rat 9.4 pKd = 9.4 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CCC/N=C(\NC#N)NCc1ccccn1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
44316759 168302 0 None - 1 Rat 9.4 pKd = 9.4 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1537 45 17 19 -0.7 CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL438191 168302 0 None - 1 Rat 9.4 pKd = 9.4 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL 1537 45 17 19 -0.7 CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CCCCNC(=O)c1cccnc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2369851 207966 0 None - 1 Rat 9.3 pKd = 9.3 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2370818 208182 0 None - 1 Human 9.3 pKd = 9.3 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
CHEMBL441741 212145 0 None - 1 Rat 9.2 pKd = 9.2 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O 10.1021/jm00398a030
CHEMBL2370808 208179 0 None - 1 Human 9.2 pKd = 9.2 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00101a003
CHEMBL439892 212104 0 None - 1 Rat 9.1 pKd = 9.1 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CSSC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
10348973 3261 50 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5432 3261 50 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
5586 3261 50 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
CHEMBL1800159 3261 50 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
DB11853 3261 50 None - 1 Human 9.1 pKd = 9.1 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 623 9 2 11 3.8 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(C)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccc(nn1)OC 10.1021/acs.jmedchem.0c01076
CHEMBL2370803 208177 0 None - 1 Human 9.1 pKd = 9.1 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CCCCNc1n[nH]c(N)n1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@@H]1C(=O)NCC(N)=O 10.1021/jm00101a003
CHEMBL2370814 208181 0 None - 1 Human 9.1 pKd = 9.1 Binding
The binding affinity towards Gonadotropin-releasing hormone receptorThe binding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CCNC(=O)CNC(=O)[C@H]1CCCN1C(=O)[C@H](CCCCNC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CCCCNc1n[nH]c(N)n1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@@H](Cc1ccc2ccccc2c1)NC(C)=O 10.1021/jm00101a003
CHEMBL407482 210917 0 None - 1 Rat 9.0 pKd = 9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](Cc1cccnc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL411806 211212 0 None - 1 Rat 9.0 pKd = 9 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)NC[C@H](NC(=O)[C@@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](Cc1ccc2ccccc2c1)NC(C)=O)c1cccnc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(N)=O)C(N)=O)c1cccnc1 10.1021/jm00398a030
CHEMBL436334 211931 0 None - 1 Rat 9.0 pKd = 9 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CCC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL2371272 208283 0 None - 1 Rat 9.0 pKd = 9.0 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CCC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
CHEMBL414149 211366 0 None - 1 Rat 9.0 pKd = 9.0 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
11250647 1516 40 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
5293 1516 40 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
8362 1516 40 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL1208155 1516 40 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
DB11979 1516 40 None 117 2 Human 8.9 pKd = 8.9 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL407023 210885 0 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@@H](NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL439359 212091 0 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@@H](CCCC/N=C(\NC#N)NC1CCCCC1)NC(=O)[C@H](CCCC/N=C(\NC#N)NC1CCCCC1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL411586 211199 0 None - 1 Rat 8.9 pKd = 8.9 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](CCCCN/C(=N/CCCC)NC#N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL412802 211279 0 None - 1 Rat 8.8 pKd = 8.8 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCCC[C@@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL2371274 208285 0 None - 1 Rat 8.7 pKd = 8.7 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
CHEMBL2371275 208286 0 None - 1 Rat 8.0 pKd = 8 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CNC(=O)C[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
CHEMBL442303 212161 0 None - 1 Rat 8.0 pKd = 8 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CNC(=O)C[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL265825 208920 0 None - 1 Rat 8.0 pKd = 8.0 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL428837 211731 0 None - 1 Rat 8.7 pKd = 8.7 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCC/N=C(\NC#N)NCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](CCCN/C(=N/CCCC)NC#N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
11250647 1516 40 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
5293 1516 40 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
8362 1516 40 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL1208155 1516 40 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
DB11979 1516 40 None 117 2 Human 8.5 pKd = 8.5 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/acs.jmedchem.0c01076
CHEMBL265522 208907 0 None - 1 Rat 8.5 pKd = 8.5 Binding
In vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranesIn vitro binding affinity of Gonadotropin-releasing hormone antagonist was measured in rat pituitary cell membranes
ChEMBL None None None CCCCCC/N=C(\NC#N)NCCCC[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](CCCCN/C(=N/CCCCCC)NC#N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCNC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@H](C)C(N)=O 10.1021/jm00112a013
CHEMBL442303 212161 0 None - 1 Rat 8.4 pKd = 8.4 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](C(=O)N[C@H]1CNC(=O)C[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](c2cccnc2)NC(=O)[C@H](CCCN=C(N)N)NC1=O)c1cccnc1 10.1021/jm00398a030
CHEMBL2371273 208284 0 None - 1 Rat 7.4 pKd = 7.4 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CC(=O)NCCC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
12784 571 8 None - 1 Human 8.3 pKd = 8.3 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 571 8 None - 1 Human 8.3 pKd = 8.3 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 571 8 None - 1 Human 8.3 pKd = 8.3 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as equilibrium dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL2371277 208288 0 None - 1 Rat 8.2 pKd = 8.2 Binding
Inhibitory binding constant for Gonadotropin-releasing hormone receptorInhibitory binding constant for Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@@H](NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2ccc(F)cc2)NC(=O)[C@H](N)Cc2ccc3ccccc3c2)CSSC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC1=O 10.1021/jm00398a030
3823 49951 38 None -1 11 Rat 6.1 pKd = 6.1 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
76973198 49951 38 None -1 11 Rat 6.1 pKd = 6.1 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
CHEMBL157101 49951 38 None -1 11 Rat 6.1 pKd = 6.1 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]leuprolide as radioligand, at concentration 3.16*10e-5 M
ChEMBL 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1021/jm00129a003
12784 571 8 None - 1 Human 8.0 pKd = 8.0 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
85469632 571 8 None - 1 Human 8.0 pKd = 8.0 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL4537788 571 8 None - 1 Human 8.0 pKd = 8.0 Binding
Inhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assayInhibition of Tag-lite green-labeled agonist binding to terbium fluorophore-labeled human N-terminal SNAP-tag GnRh receptor expressed in HEK293 cells assessed as dissociation constant by TR-FRET assay
ChEMBL 671 6 1 6 5.3 ClC1=C(CNC(C2=CC=C3N(S(=O)(C4=CC=C(F)C=C4)=O)[C@@H](C5CC5)C6(CCS(CC6)(=O)=O)C3=C2)=O)N=CC(C(F)(F)F)=C1 10.1021/acs.jmedchem.0c01076
CHEMBL409219 211007 0 None - 1 Rat 10.9 pKi = 10.9 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL268397 209006 0 None - 1 Rat 10.6 pKi = 10.6 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
44383749 96220 0 None - 1 Rat 10.5 pKi = 10.5 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1534 41 13 18 3.1 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC(N)C(=O)c1ccncc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL263839 96220 0 None - 1 Rat 10.5 pKi = 10.5 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1534 41 13 18 3.1 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N(C)[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCC(N)C(=O)c1ccncc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL263840 208846 0 None - 1 Rat 10.5 pKi = 10.5 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1csc2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL268319 209000 0 None - 1 Rat 10.3 pKi = 10.3 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None COc1ccc(C(=O)CC[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CO)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(C)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)cc1 10.1021/jm00059a020
44383968 158776 0 None - 1 Rat 10.2 pKi = 10.2 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1590 45 14 20 2.5 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL409990 158776 0 None - 1 Rat 10.2 pKi = 10.2 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL 1590 45 14 20 2.5 CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CCCC(N)C(=O)c1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCC(N)C(C)C)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL2371478 208306 0 None - 1 Rat 10.0 pKi = 10 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3c[nH]cn3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44267907 16155 0 None 3 3 Rat 10.0 pKi = 10.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12282 16155 0 None 3 3 Rat 10.0 pKi = 10.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL438829 212053 0 None - 1 Rat 9.9 pKi = 9.9 Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptorThe negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@@H]1C(=O)N[C@@H](C)C(N)=O 10.1021/jm00059a020
CHEMBL2371592 208357 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCNC(=O)CNC(=O)CC[C@H](NC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990116+
CHEMBL386166 210630 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL405548 210818 0 None - 1 Human 9.9 pKi = 9.9 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCNC(=O)CNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990118u
CHEMBL2371557 208338 0 None - 1 Rat 9.9 pKi = 9.9 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44379996 96392 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CC(=O)NCCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
91931282 96392 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CC(=O)NCCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL265240 96392 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CC(=O)NCCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44378966 95997 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL262160 95997 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL2371516 208322 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371582 208350 0 None - 1 Rat 9.8 pKi = 9.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371533 208329 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
11364940 177950 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 555 8 1 8 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL466731 177950 0 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 555 8 1 8 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
1185 3645 32 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
3038517 3645 32 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
CHEMBL22055 3645 32 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
DB06494 3645 32 None - 1 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 10.1016/s0960-894x(03)00746-7
1184 3676 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
9874838 3676 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
CHEMBL71917 3676 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
CHEMBL2371483 208308 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCNC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371485 208310 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](CCCN=C(N)N)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371515 208321 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CN(C)C(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
23656390 161134 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL413245 161134 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 659 10 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
1184 3676 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting methodDisplacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting method
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
9874838 3676 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting methodDisplacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting method
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL71917 3676 31 None 426 2 Human 9.7 pKi = 9.7 Binding
Displacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting methodDisplacement of [125I]leuprorelin from human GnRHR expressed in CHO cell membranes after 60 mins by gamma-ray counting method
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1039/C7MD00320J
CHEMBL407361 210910 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)N[C@H](C)C(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL439083 212071 0 None - 1 Rat 9.7 pKi = 9.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371514 208320 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL2371522 208326 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccc(Cl)cc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44267812 97652 0 None 7 3 Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273440 97652 0 None 7 3 Rat 9.6 pKi = 9.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL438897 212056 0 None -1 2 Rat 9.6 pKi = 9.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL438897 212056 0 None 1 2 Human 9.6 pKi = 9.6 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990118u
CHEMBL436657 211936 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL406809 210873 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Affinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371591 208356 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CC=C[C@H]1C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm990116+
CHEMBL269726 209059 0 None - 1 Human 9.6 pKi = 9.6 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CC=C[C@@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(O)cc2)NC1=O 10.1021/jm990118u
CHEMBL2371507 208317 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCNC(=O)[C@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44379287 160869 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1299 26 14 15 -1.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL412681 160869 0 None - 1 Rat 9.6 pKi = 9.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1299 26 14 15 -1.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44449120 94789 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 94789 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44432648 149694 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL395225 149694 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 643 9 2 4 7.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4nccnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL411964 211218 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371537 208330 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CC[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
CHEMBL2371587 208354 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990116+
CHEMBL441208 212138 0 None - 1 Human 9.5 pKi = 9.5 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990118u
CHEMBL2371566 208343 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CCNC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
44378889 168591 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1251 27 13 16 -2.8 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H]1CC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL440436 168591 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1251 27 13 16 -2.8 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H]1CC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL2371519 208325 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44267907 16155 0 None -3 3 Human 9.5 pKi = 9.5 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL12282 16155 0 None -3 3 Human 9.5 pKi = 9.5 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267907 16155 0 None -3 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12282 16155 0 None -3 3 Human 9.5 pKi = 9.5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 937 11 1 14 6.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL2371568 208344 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371578 208347 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)NCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371517 208323 0 None - 1 Rat 9.5 pKi = 9.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CNC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44448991 154802 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154802 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154802 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL2371470 208305 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL2371486 208311 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)CCNC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL410779 211092 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
9872676 77826 0 None 1 17 Human 9.4 pKi = 9.4 Binding
Binding affinity to human recombinant GnRH receptorBinding affinity to human recombinant GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 77826 0 None 1 17 Human 9.4 pKi = 9.4 Binding
Binding affinity to human recombinant GnRH receptorBinding affinity to human recombinant GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
9872676 77826 0 None -1 17 Rat 9.4 pKi = 9.4 Binding
Binding affinity to rat pituitary GnRH receptorBinding affinity to rat pituitary GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
CHEMBL210514 77826 0 None -1 17 Rat 9.4 pKi = 9.4 Binding
Binding affinity to rat pituitary GnRH receptorBinding affinity to rat pituitary GnRH receptor
ChEMBL 565 11 2 10 4.8 COc1nc(NCCCN2CCOCC2)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1021/jm060012g
10649568 14397 0 None 10 2 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
CHEMBL120432 14397 0 None 10 2 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
9961721 167914 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL435167 167914 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 7 7.0 CCNC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44432647 86313 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231954 86313 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 622 9 2 4 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(=O)n(C)c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL216634 207590 0 None - 1 Rat 9.4 pKi = 9.4 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11376252 69028 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
CHEMBL192955 69028 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
11376252 69028 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL192955 69028 0 None - 1 Human 9.4 pKi = 9.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 547 7 1 6 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL2371577 208346 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL429007 211744 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11421412 178164 11 None 2398 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL468551 178164 11 None 2398 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44388510 165687 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 538 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1F 10.1021/jm049218c
CHEMBL426780 165687 0 None - 1 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 538 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1F 10.1021/jm049218c
11421412 178164 11 None 2398 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL468551 178164 11 None 2398 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44432651 86276 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231760 86276 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 632 9 3 4 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44432643 146234 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392446 146234 0 None - 1 Rat 9.3 pKi = 9.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 592 9 2 3 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11167850 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1178 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1187 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL179691 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
11167850 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
11167850 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
1178 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
1187 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
CHEMBL179691 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2008.04.029
11167850 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
1178 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
1187 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
CHEMBL179691 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1016/j.bmcl.2005.03.057
11167850 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1178 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1187 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL179691 2701 22 None 6309 2 Human 9.3 pKi = 9.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL2371579 208348 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@@H](C)NC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
CHEMBL2371508 208318 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](CCCN=C(N)N)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
11443711 10037 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL115703 10037 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
44346397 114000 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL333518 114000 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 639 10 0 9 6.2 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44432652 96693 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL267838 96693 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 633 9 3 5 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cnc4[nH]nnc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44432654 159248 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL410547 159248 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 660 10 3 6 6.1 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(-c4nnn[nH]4)nc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44400235 167867 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
CHEMBL434936 167867 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
10345138 122042 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 122042 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 122042 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
44449681 95599 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL259906 95599 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
9854500 101802 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
CHEMBL303274 101802 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the rat Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
9854500 101802 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
CHEMBL303274 101802 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm701249f
44400235 167867 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL434936 167867 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44400235 167867 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL434936 167867 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44400235 167867 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL434936 167867 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44400235 167867 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL434936 167867 0 None - 1 Human 9.2 pKi = 9.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
9854500 101802 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL303274 101802 0 None 1 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
44267887 98029 0 None -5 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275935 98029 0 None -5 3 Rat 9.2 pKi = 9.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
10345138 122042 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm701249f
CHEMBL360143 122042 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm701249f
CHEMBL75347 122042 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm701249f
44448991 154802 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154802 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154802 0 None - 1 Human 9.2 pKi = 9.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
10345138 122042 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL360143 122042 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL75347 122042 0 None 2041 2 Human 9.2 pKi = 9.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL2371541 208333 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CNC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
44432653 86277 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231761 86277 0 None - 1 Rat 9.2 pKi = 9.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 650 9 3 4 6.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2cc4nn[nH]c4cc2F)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451355 157621 0 None - 1 Human 9.2 pKi = 9.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 577 11 2 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(C)CNCCCCc2ccnnc2)c1 10.1016/j.bmc.2007.09.026
CHEMBL408746 157621 0 None - 1 Human 9.2 pKi = 9.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 577 11 2 4 7.4 Cc1cc(C)cc(-c2[nH]c3ccc(C(C)(C)C(=O)N4C5CCC4CC5)cc3c2C(C)CNCCCCc2ccnnc2)c1 10.1016/j.bmc.2007.09.026
CHEMBL2371502 208316 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@](C)(Cc2ccc(O)cc2)NC1=O 10.1021/jm990115h
CHEMBL2371484 208309 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCNC(=O)[C@H](Cc3ccccc3)NC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44380258 160710 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CCC(=O)NCCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
91931283 160710 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CCC(=O)NCCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL411963 160710 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1441 14 16 15 -2.1 CC(=O)N[C@@H]1CCC(=O)NCCC(=O)NC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
10985312 78336 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL21126 78336 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
10985312 78336 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/j.bmc.2007.09.026
CHEMBL21126 78336 0 None - 1 Human 9.1 pKi = 9.1 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 650 10 1 7 7.2 CCC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/j.bmc.2007.09.026
CHEMBL2371575 208345 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL405420 210812 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44288080 159641 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 1009 15 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL410940 159641 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 1009 15 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(F)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL407800 210937 0 None - 1 Rat 9.1 pKi = 9.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44400245 125560 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL364914 125560 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44400245 125560 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL364914 125560 0 None - 1 Human 9.1 pKi = 9.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 541 8 1 8 3.1 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
11250647 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
5293 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
8362 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
CHEMBL1208155 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
DB11979 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
44400271 68986 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL192912 68986 0 None - 1 Human 9.0 pKi = 9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1016/j.bmcl.2005.03.057
CHEMBL2371549 208335 0 None - 1 Rat 9.0 pKi = 9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CN)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC1=O 10.1021/jm990115h
44432649 86272 0 None - 1 Rat 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL231739 86272 0 None - 1 Rat 9.0 pKi = 9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 3 7.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc4[nH]c(C)nc4c2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11365653 173618 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL454774 173618 0 None - 1 Human 9.0 pKi = 9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
10311600 160361 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 523 10 3 9 4.4 CNCCNc1nc(OC)c(NC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)OC4(C)C)o2)c(OC)n1 10.1016/j.bmc.2007.09.026
CHEMBL411526 160361 0 None - 1 Human 9.0 pKi = 9 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 523 10 3 9 4.4 CNCCNc1nc(OC)c(NC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)OC4(C)C)o2)c(OC)n1 10.1016/j.bmc.2007.09.026
CHEMBL385982 210625 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL410357 211068 0 None - 1 Rat 9.0 pKi = 9.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCCCC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11477988 90579 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm701249f
CHEMBL23969 90579 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm701249f
11477988 90579 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 90579 0 None 954 2 Human 9.0 pKi = 9.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
21018389 67123 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL189164 67123 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353277 20070 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 712 16 2 7 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL130558 20070 0 None - 1 Human 9.0 pKi = 9.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 712 16 2 7 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
25156943 187853 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL502341 187853 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 597 12 2 7 5.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
21036877 173078 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL453441 173078 0 None - 1 Human 9.0 pKi = 9.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44340749 108631 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL321376 108631 0 None - 1 Human 9.0 pKi = 9.0 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
44267868 97624 0 None 10 2 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273275 97624 0 None 10 2 Rat 8.9 pKi = 8.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
9809065 101160 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 611 11 0 9 5.2 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccn1 10.1021/jm0205402
CHEMBL298982 101160 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 611 11 0 9 5.2 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccn1 10.1021/jm0205402
11202636 10135 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL116071 10135 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44353248 19552 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 13 1 8 5.9 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL130126 19552 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 13 1 8 5.9 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
11202636 10135 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL116071 10135 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 9 1 6 4.1 CN[C@H](CC(C)C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
21018389 67123 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL189164 67123 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 1 5 5.2 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44379167 167199 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL 1376 16 15 15 -1.0 CC(=O)NC1CC(=O)NC(C(=O)N[C@H]2CC(=O)NC(C(=O)O)CNC(=O)[C@@H]3CCCN3C(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)C(Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL430344 167199 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL 1376 16 15 15 -1.0 CC(=O)NC1CC(=O)NC(C(=O)N[C@H]2CC(=O)NC(C(=O)O)CNC(=O)[C@@H]3CCCN3C(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)C(Cc3ccc4ccccc4c3)NC(=O)[C@H](Cc3ccc(O)cc3)NC2=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371487 208312 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
11331001 188435 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL509075 188435 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
21036878 172477 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 5.9 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL451916 172477 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 5.9 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
11365653 173618 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL454774 173618 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 2 7 5.7 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
11331001 188435 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
CHEMBL509075 188435 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.07.059
11262242 188152 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL505033 188152 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44288081 157779 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 13 1 14 8.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL408925 157779 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 13 1 14 8.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(CC3CC3)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44400261 133491 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
CHEMBL371613 133491 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
44400261 133491 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
CHEMBL371613 133491 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 527 7 1 7 3.6 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
44378649 96706 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1287 27 14 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
CHEMBL267984 96706 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1287 27 14 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H]1CCC(=O)N(CC(N)=O)C(=O)[C@H]2CCCN2C(=O)[C@H](CCCCN)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CCC(=O)O)NC1=O 10.1021/jm990115h
44379259 141072 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1277 24 12 15 -0.4 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
CHEMBL385090 141072 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1277 24 12 15 -0.4 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
44378908 161283 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1273 27 14 15 -2.3 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)N(CC(=O)O)C(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm990115h
CHEMBL414556 161283 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1273 27 14 15 -2.3 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)N(CC(=O)O)C(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(N)=O)NC1=O 10.1021/jm990115h
CHEMBL2371518 208324 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCCCNC(=O)CC[C@H](NC1=O)C(=O)N[C@H](Cc1ccc3ccccc3c1)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
44432635 86356 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232150 86356 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 512 8 2 3 6.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2C(C)(C)C2(C)C)CC3)c1 10.1016/j.bmcl.2007.05.009
11262242 188152 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL505033 188152 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 645 13 2 7 6.1 Cc1c(-c2cccc(OCCCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44434386 89378 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL237734 89378 0 None - 1 Human 8.9 pKi = 8.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 638 11 2 8 5.1 C#CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
86276160 109366 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 485 9 1 8 5.0 COc1nc(OCCF)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
CHEMBL3233521 109366 0 None - 1 Rat 8.9 pKi = 8.9 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 485 9 1 8 5.0 COc1nc(OCCF)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
44400229 68341 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL192171 68341 0 None - 1 Human 8.9 pKi = 8.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 497 7 1 6 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL2371559 208340 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44432636 86957 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233341 86957 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 550 8 2 3 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C24CC5CC(CC(C5)C2)C4)CC3)c1 10.1016/j.bmcl.2007.05.009
44432642 153060 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL398060 153060 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 574 9 2 3 6.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44287759 96249 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 999 12 2 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL264043 96249 0 None - 1 Human 8.8 pKi = 8.8 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 999 12 2 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL407589 210923 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)N[C@@H](C)C(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL410382 211070 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3cccnc3)NC2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371538 208331 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44347047 16422 0 None 5 2 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL124056 16422 0 None 5 2 Rat 8.8 pKi = 8.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL264332 208868 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL2371531 208327 0 None - 1 Rat 8.8 pKi = 8.8 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CNC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)C[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC1=O 10.1021/jm9901172
CHEMBL412009 211223 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCCC[C@@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11168776 63279 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL180076 63279 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44400352 67459 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 545 8 1 6 5.1 CCOc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL190929 67459 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 545 8 1 6 5.1 CCOc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL2371539 208332 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](C)NC(=O)C[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
44378966 95997 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL262160 95997 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1336 26 15 17 -3.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCC(=O)NC(=O)CC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44432650 86344 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
CHEMBL232097 86344 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 703 10 3 5 6.5 CCn1c(=O)[nH]c2cc(CCNC[C@@H](C)c3c(-c4cc(C)cc(C)c4)[nH]c4c3CN(C(=O)Cc3c(F)cccc3C(F)(F)F)CC4)ccc2c1=O 10.1016/j.bmcl.2007.05.009
44432640 154434 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401226 154434 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 524 9 2 3 5.9 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2F)CC3)c1 10.1016/j.bmcl.2007.05.009
9854500 101802 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL303274 101802 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
9854500 101802 0 None -2 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL303274 101802 0 None -2 3 Human 8.7 pKi = 8.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
9854500 101802 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
CHEMBL303274 101802 0 None -2 3 Human 8.7 pKi = 8.7 Binding
Ability of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility of compound to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 953 11 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/s0960-894x(02)00370-0
11331001 188435 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL509075 188435 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44576645 187613 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 571 9 2 8 3.6 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499026 187613 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 571 9 2 8 3.6 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353201 20847 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 15 2 7 6.3 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL131182 20847 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 15 2 7 6.3 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44394589 66586 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 453 6 1 6 4.1 Cc1c(-c2cccs2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL186563 66586 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 453 6 1 6 4.1 Cc1c(-c2cccs2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11752130 14023 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL119808 14023 0 None - 1 Human 8.0 pKi = 8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL405806 210836 0 None - 1 Rat 8.0 pKi = 8 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H]1CC(=O)NCC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](CCCCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](CCC(=O)O)NC1=O 10.1021/jm990115h
44435979 88113 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL235269 88113 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44436017 88304 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 9 0 7 4.7 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236152 88304 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 9 0 7 4.7 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44435993 161132 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 665 10 0 8 5.9 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3C(F)(F)F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL413238 161132 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 665 10 0 8 5.9 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3C(F)(F)F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44347085 15083 0 None -3 2 Human 8.0 pKi = 8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121145 15083 0 None -3 2 Human 8.0 pKi = 8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44587396 172685 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 603 10 2 7 4.9 Cc1c(-c2cccc(OCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL452474 172685 0 None - 1 Human 8.0 pKi = 8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 603 10 2 7 4.9 Cc1c(-c2cccc(OCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44343914 114311 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL334063 114311 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11330603 128156 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL366865 128156 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL430613 128156 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
11156980 62264 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL178281 62264 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44353229 19990 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 11 1 7 6.5 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130487 19990 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 11 1 7 6.5 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44343914 114311 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL334063 114311 0 None - 1 Human 7.0 pKi = 7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 635 13 0 9 6.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
44309615 102196 0 None - 1 Human 7.0 pKi = 7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(Cl)cc(Cl)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304548 102196 0 None - 1 Human 7.0 pKi = 7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(Cl)cc(Cl)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44435978 88069 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 575 11 0 8 3.5 COc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL235051 88069 0 None - 1 Human 7.0 pKi = 7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 575 11 0 8 3.5 COc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
11284357 60692 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL176270 60692 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL72913 60692 0 None - 1 Human 6.0 pKi = 6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1016/j.bmcl.2004.02.004
44451476 95400 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1535 30 8 18 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL258970 95400 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1535 30 8 18 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44267883 16137 0 None -3 2 Human 5.0 pKi = 5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12265 16137 0 None -3 2 Human 5.0 pKi = 5 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11249548 98633 0 None -97 2 Rat 5.0 pKi = 5 Binding
In vivo inhibition of rat Gonadotropin releasing hormone receptorIn vivo inhibition of rat Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 98633 0 None -97 2 Rat 5.0 pKi = 5 Binding
In vivo inhibition of rat Gonadotropin releasing hormone receptorIn vivo inhibition of rat Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
44340637 9488 0 None 1479 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards monkey gonadotropin releasing hormone receptorBinding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112466 9488 0 None 1479 2 Human 7.0 pKi = 7.0 Binding
Binding affinity towards monkey gonadotropin releasing hormone receptorBinding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21048269 110608 0 None 2 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326313 110608 0 None 2 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21047785 15285 0 None 20 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121576 15285 0 None 20 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11227010 85238 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 12 0 9 3.9 COc1cc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc(OC)c1OC 10.1021/jm030472z
CHEMBL22852 85238 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 12 0 9 3.9 COc1cc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc(OC)c1OC 10.1021/jm030472z
CHEMBL438103 212002 0 None - 1 Rat 8.0 pKi = 8.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCCC[C@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC1=O 10.1021/jm990116+
9807700 186719 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 8 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL49297 186719 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 8 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44346376 113307 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 10 1 7 7.3 CCNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL332463 113307 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 10 1 7 7.3 CCNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44309440 102161 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304308 102161 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44387924 60156 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175465 60156 0 None - 1 Human 8.0 pKi = 8.0 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047534 16264 0 None 1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL123284 16264 0 None 1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
21047534 16264 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL123284 16264 0 None -1 2 Rat 8.0 pKi = 8.0 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 609 13 3 7 7.3 COCCCNc1ccnc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL263542 208829 0 None - 1 Rat 7.0 pKi = 7.0 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC1=O 10.1021/jm990116+
12986401 187058 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 464 7 1 7 3.0 COc1cccc(-n2c(=O)c(Cc3c(F)cccc3F)nn(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
CHEMBL494968 187058 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 464 7 1 7 3.0 COc1cccc(-n2c(=O)c(Cc3c(F)cccc3F)nn(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
10226423 188819 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)[C@@H](c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
CHEMBL513126 188819 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)[C@@H](c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
11330034 83980 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2ccc(C(C)C)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22196 83980 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2ccc(C(C)C)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44593613 188074 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
CHEMBL503624 188074 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
44389658 62916 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL179101 62916 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
44309541 202176 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 647 12 0 9 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68753 202176 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 647 12 0 9 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44309439 202208 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 630 10 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68988 202208 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 630 10 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
44593613 188074 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.07.059
CHEMBL503624 188074 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 598 11 2 8 4.2 CCOC(=O)CNCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.07.059
21045834 16268 0 None 3 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL123301 16268 0 None 3 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44451367 59354 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 6 1 6 4.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4NCCc5ccccc54)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
CHEMBL172192 59354 0 None - 1 Human 7.0 pKi = 7.0 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 6 1 6 4.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4NCCc5ccccc54)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
9892420 201451 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL64148 201451 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11294757 63507 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL180280 63507 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
44576643 187470 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 512 7 2 6 4.0 NCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
CHEMBL497747 187470 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 512 7 2 6 4.0 NCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
11329628 62695 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1016/j.bmcl.2004.02.004
CHEMBL178805 62695 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1016/j.bmcl.2004.02.004
CHEMBL73575 62695 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1016/j.bmcl.2004.02.004
10983979 201485 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 505 10 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccc3)c2=O)c1 10.1021/jm034041s
CHEMBL64252 201485 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 505 10 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccc3)c2=O)c1 10.1021/jm034041s
44451485 157630 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2cccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL408759 157630 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2cccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11226753 63014 0 None -389 2 Rat 5.0 pKi = 5.0 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 63014 0 None -389 2 Rat 5.0 pKi = 5.0 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
9984259 110012 0 None -281 2 Rat 5.0 pKi = 5.0 Binding
Tested for binding affinity towards rat gonadotropin releasing hormone receptorTested for binding affinity towards rat gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL324912 110012 0 None -281 2 Rat 5.0 pKi = 5.0 Binding
Tested for binding affinity towards rat gonadotropin releasing hormone receptorTested for binding affinity towards rat gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
44267881 17889 0 None 14 2 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12666 17889 0 None 14 2 Rat 7.0 pKi = 7.0 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44267876 97655 0 None -53 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273466 97655 0 None -53 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44309511 202553 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 624 13 1 9 5.3 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL71141 202553 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 624 13 1 9 5.3 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
44340788 9451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112287 9451 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44343804 10472 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 517 10 1 6 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](CC(C)C)NC(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL116976 10472 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 517 10 1 6 4.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](CC(C)C)NC(C)C)c2=O)c1F 10.1021/jm049791w
44343779 10919 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL117504 10919 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL2371488 208313 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@H](Cc3ccccc3)NC(=O)C[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
25156946 187785 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 11 2 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL501329 187785 0 None - 1 Human 7.9 pKi = 7.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 617 11 2 7 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11168634 84664 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 536 10 0 7 4.6 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL22459 84664 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 536 10 0 7 4.6 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
11226753 63014 0 None 389 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 63014 0 None 389 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11180219 110733 0 None 112 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 110733 0 None 112 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
44394723 123825 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 468 6 1 7 3.8 Cc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL363659 123825 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 468 6 1 7 3.8 Cc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
44400146 67231 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 570 9 1 8 3.0 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL189984 67231 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 570 9 1 8 3.0 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL2371493 208314 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]2CCNC(=O)[C@@H](Cc3ccccc3)NC(=O)CC[C@H](NC1=O)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@@H](CC(C)C)C(=O)N2 10.1021/jm990115h
CHEMBL265232 208896 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44432627 147596 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL393540 147596 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 430 7 2 3 4.5 CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
44387880 60214 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL175821 60214 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
44387979 60278 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 8 1 9 2.1 COc1ccccc1Cn1c(=O)n(C[C@H](N)c2ccccc2)c(=O)n(-c2cccc(OC)c2F)c1=O 10.1016/j.bmcl.2005.05.038
CHEMBL176020 60278 0 None - 1 Human 6.9 pKi = 6.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 8 1 9 2.1 COc1ccccc1Cn1c(=O)n(C[C@H](N)c2ccccc2)c(=O)n(-c2cccc(OC)c2F)c1=O 10.1016/j.bmcl.2005.05.038
23450008 131885 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL369723 131885 0 None - 1 Human 6.9 pKi = 6.9 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
44267904 97964 0 None 6 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275521 97964 0 None 6 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44352734 18329 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL127384 18329 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11443571 164260 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2cccc(F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL421858 164260 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2cccc(F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11168176 122506 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL360910 122506 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL73526 122506 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
21047799 109914 0 None -6 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL324394 109914 0 None -6 2 Rat 5.9 pKi = 5.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340631 9417 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112131 9417 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
11421412 178164 11 None -2398 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL468551 178164 11 None -2398 2 Rat 5.9 pKi = 5.9 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 545 7 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
11763365 100733 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 551 7 0 7 5.4 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc4c(n3c2=O)CN(CCc2ccccn2)CC4(C)C)c1 10.1021/jm0205402
CHEMBL295807 100733 0 None - 1 Human 4.9 pKi = 4.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 551 7 0 7 5.4 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc4c(n3c2=O)CN(CCc2ccccn2)CC4(C)C)c1 10.1021/jm0205402
9984259 110012 0 None -281 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 110012 0 None -281 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44309440 102161 0 None - 1 Human 4.9 pKi = 4.9 Binding
Compound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistCompound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304308 102161 0 None - 1 Human 4.9 pKi = 4.9 Binding
Compound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistCompound was evaluated in cloned rat Gonadotropin-releasing hormone receptor assay for its ability to displace the binding of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44267903 161683 0 None 3 2 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL416337 161683 0 None 3 2 Rat 5.9 pKi = 5.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44389652 165471 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 473 6 1 7 3.5 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1F 10.1016/j.bmcl.2005.01.009
CHEMBL425529 165471 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 473 6 1 7 3.5 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1F 10.1016/j.bmcl.2005.01.009
10347081 89080 0 None -223 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23730 89080 0 None -223 2 Rat 4.9 pKi = 4.9 Binding
Binding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards rat gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
44435817 88675 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 489 6 0 6 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL236544 88675 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 489 6 0 6 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL410452 211076 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
CHEMBL438901 212057 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm990116+
44577101 177952 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 532 7 1 7 4.1 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL466736 177952 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 532 7 1 7 4.1 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
11249548 98633 0 None 97 2 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 98633 0 None 97 2 Human 7.9 pKi = 7.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
11179420 63019 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 6 4.7 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1021/jm049218c
CHEMBL179460 63019 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 6 4.7 CSc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1021/jm049218c
11341364 165533 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 519 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL425864 165533 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 519 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44388018 60152 0 None 389 2 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 60152 0 None 389 2 Human 7.9 pKi = 7.9 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
10050123 11078 0 None 20 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117863 11078 0 None 20 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44288074 99764 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 951 13 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL288534 99764 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 951 13 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
11179660 89282 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23767 89282 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
10930118 101489 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 610 11 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccc1 10.1021/jm0205402
CHEMBL301322 101489 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 610 11 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)CCc1ccccc1 10.1021/jm0205402
11179660 89282 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL23767 89282 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
44353254 21608 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 574 12 1 7 6.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)C)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL131942 21608 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 574 12 1 7 6.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)C)cc1 10.1016/s0960-894x(01)00780-6
44394651 122410 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 573 8 2 8 5.8 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)c(C)c1 10.1016/j.bmcl.2004.07.022
CHEMBL360625 122410 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 573 8 2 8 5.8 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)c(C)c1 10.1016/j.bmcl.2004.07.022
44394685 126983 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL366127 126983 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
10951713 101778 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL303140 101778 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
44309573 201970 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 625 12 0 9 5.8 CCN(CC)CCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL67370 201970 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 625 12 0 9 5.8 CCN(CC)CCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL405961 210841 0 None - 1 Rat 6.9 pKi = 6.9 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
21045818 112597 0 None 3 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331337 112597 0 None 3 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44388018 60152 0 None -389 2 Rat 4.9 pKi = 4.9 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 60152 0 None -389 2 Rat 4.9 pKi = 4.9 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44436014 88158 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 568 7 0 6 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1C1CCCC1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL235519 88158 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 568 7 0 6 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1C1CCCC1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44436016 147040 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 688 10 0 8 5.3 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCN(C[C@@H]3CCCN3Cc3ccccn3)C1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL393093 147040 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 688 10 0 8 5.3 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCN(C[C@@H]3CCCN3Cc3ccccn3)C1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44309535 102517 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL306684 102517 0 None - 1 Human 7.9 pKi = 7.9 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
44379747 96337 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990116+
CHEMBL264806 96337 0 None -1 2 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990116+
CHEMBL410451 211075 0 None - 1 Rat 7.9 pKi = 7.9 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
44577097 177916 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.4 C=C1C(Cl)=CC=C1c1c(C)n(Cc2c(F)cccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm701249f
CHEMBL466531 177916 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 6 1 5 4.4 C=C1C(Cl)=CC=C1c1c(C)n(Cc2c(F)cccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm701249f
11261693 63078 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1021/jm049218c
CHEMBL179612 63078 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1021/jm049218c
CHEMBL74721 63078 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1021/jm049218c
44353270 114716 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 12 1 8 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL334537 114716 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 623 12 1 8 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44353230 116286 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 610 13 0 8 6.4 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL337748 116286 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 610 13 0 8 6.4 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44379747 96337 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990118u
CHEMBL264806 96337 0 None 1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity towards Gonadotropin-releasing hormone receptorBinding affinity towards Gonadotropin-releasing hormone receptor
ChEMBL 1350 15 13 13 1.4 CC(C)C[C@H]1C(=O)N[C@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)NCCC(=O)N2CC=C[C@H]2C(=O)N[C@@H](Cc2ccc(Cl)cc2)C(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)N[C@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N1C 10.1021/jm990118u
44394567 65851 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccc(Cl)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL184345 65851 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccc(Cl)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
21047618 114032 0 None -1 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333574 114032 0 None -1 2 Human 7.9 pKi = 7.9 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44267874 96766 0 None 15 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268489 96766 0 None 15 2 Rat 7.9 pKi = 7.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11283517 95010 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL25714 95010 0 None - 1 Human 6.9 pKi = 6.9 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11283517 95010 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL25714 95010 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1 10.1021/jm030472z
11330280 122536 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1021/jm049218c
CHEMBL360934 122536 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1021/jm049218c
CHEMBL72606 122536 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1021/jm049218c
21047937 110809 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326606 110809 0 None -1 2 Rat 6.9 pKi = 6.9 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44312724 12294 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C(C)c1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL1185733 12294 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C(C)c1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL430618 12294 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C(C)c1ccccc1 10.1016/j.bmcl.2004.02.004
44309616 202048 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(C(F)(F)F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL67820 202048 0 None - 1 Human 6.9 pKi = 6.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 655 10 0 7 7.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(C(F)(F)F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
25113693 161365 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL415279 161365 0 None - 1 Human 6.9 pKi = 6.9 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 896 15 3 10 6.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccccc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047859 14048 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL119856 14048 0 None 1 2 Human 6.9 pKi = 6.9 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11376064 166586 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL429062 166586 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44400147 67316 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 612 9 1 9 2.7 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N3CCOCC3)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL190676 67316 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 612 9 1 9 2.7 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)N3CCOCC3)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44309403 202207 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccncc2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68985 202207 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 631 10 0 9 6.1 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccncc2)cc1 10.1016/s0960-894x(02)00371-2
44435994 146510 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 482 8 0 6 3.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)C)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL392688 146510 0 None - 1 Human 5.9 pKi = 5.9 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 482 8 0 6 3.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)C)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44267811 96767 0 None 14 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268491 96767 0 None 14 2 Rat 6.9 pKi = 6.9 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
21047807 112487 0 None -23 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331087 112487 0 None -23 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11249167 89869 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23854 89869 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL216526 207585 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H]1CCC(=O)NCCCC[C@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc3ccc4ccccc4c3)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990116+
44435979 88113 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1021/jm701249f
CHEMBL235269 88113 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 591 11 0 8 4.2 CSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1021/jm701249f
11249167 89869 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL23854 89869 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm701249f
11214860 84347 0 None 323 2 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 84347 0 None 323 2 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
11249167 89869 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23854 89869 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
11192229 122603 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL361128 122603 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11168776 63279 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL180076 63279 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.4 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44394661 65779 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccc(Cl)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL183938 65779 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccc(Cl)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44435982 57791 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 12 0 8 4.6 CCSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL16745 57791 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 605 12 0 8 4.6 CCSc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44435986 96058 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 615 10 0 8 5.0 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL262579 96058 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 615 10 0 8 5.0 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44587398 188448 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 659 13 1 7 6.3 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@@H](c2ccccc2)N(C)C)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL509267 188448 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 659 13 1 7 6.3 Cc1c(-c2cccc(OCCCCC(=O)O)c2F)c(=O)n(C[C@@H](c2ccccc2)N(C)C)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
11214860 84347 0 None 323 2 Human 7.8 pKi = 7.8 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 84347 0 None 323 2 Human 7.8 pKi = 7.8 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
44267812 97652 0 None -64 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273440 97652 0 None -64 3 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 941 10 1 14 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
44394753 122786 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3cccc(C(F)(F)F)c3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL361513 122786 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3cccc(C(F)(F)F)c3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44346261 113370 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 651 10 2 8 5.7 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL332570 113370 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 651 10 2 8 5.7 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44340720 9616 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL113183 9616 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309296 201887 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 584 10 0 9 5.1 COCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL66808 201887 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 584 10 0 9 5.1 COCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
21045833 113192 0 None 11 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL332305 113192 0 None 11 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11330072 86509 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23231 86509 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.0 COCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
44394835 122118 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 539 7 1 9 3.3 Cc1c(-c2csc(N3CCOCC3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL360384 122118 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 539 7 1 9 3.3 Cc1c(-c2csc(N3CCOCC3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44387885 131774 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 8 2.4 COc1cccc(-n2c(=O)n(CC[C@H](N)CC(C)C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL369706 131774 0 None - 1 Human 5.8 pKi = 5.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 8 2.4 COc1cccc(-n2c(=O)n(CC[C@H](N)CC(C)C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44341075 9815 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 427 5 1 6 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCNC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114370 9815 0 None - 1 Human 4.8 pKi = 4.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 427 5 1 6 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCNC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44353266 116587 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 635 14 2 6 6.9 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL339273 116587 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 635 14 2 6 6.9 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
21045817 114052 0 None -22 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333730 114052 0 None -22 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44587401 187650 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 14 3 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL499442 187650 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 14 3 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
21048323 167149 0 None -8 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL430250 167149 0 None -8 2 Rat 5.8 pKi = 5.8 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44435819 88765 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 490 6 0 7 3.3 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccncc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL236750 88765 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 490 6 0 7 3.3 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccncc2)CC3)c1 10.1016/j.bmc.2007.05.029
11225960 10906 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL117396 10906 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
11225960 10906 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL117396 10906 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
44346375 15190 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 690 9 1 7 7.3 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)C(F)(F)F)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL121441 15190 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 690 9 1 7 7.3 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)C(F)(F)F)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
9891852 10000 0 None 23 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115482 10000 0 None 23 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9959327 101486 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 9 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL301285 101486 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 553 9 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44394714 122113 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 590 9 2 10 5.1 Cc1c(-c2csc(Nc3ccc([N+](=O)[O-])cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL360363 122113 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 590 9 2 10 5.1 Cc1c(-c2csc(Nc3ccc([N+](=O)[O-])cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
10347081 89080 0 None 223 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23730 89080 0 None 223 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards monkey gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
44436009 88931 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccc5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236966 88931 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.4 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccc5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44340845 9777 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114183 9777 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44432656 158612 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL409825 158612 0 None - 1 Rat 5.8 pKi = 5.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 645 9 3 5 6.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44451397 95458 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL259220 95458 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 856 16 4 10 5.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44434373 89617 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL238160 89617 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 637 11 3 7 4.6 C#CCNC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44267881 17889 0 None -14 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12666 17889 0 None -14 2 Human 5.8 pKi = 5.8 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 877 10 1 12 6.9 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL406628 210869 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
CHEMBL415179 211430 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCCC[C@H]2NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C2=O)NC1=O 10.1021/jm990116+
44353276 116724 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 697 15 2 6 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL339468 116724 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 697 15 2 6 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCCc4ccccc4)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
44346479 113626 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 11 1 7 7.9 CC(C)CNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL332837 113626 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 650 11 1 7 7.9 CC(C)CNc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44435977 88298 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236127 88298 0 None - 1 Human 7.8 pKi = 7.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
9911446 10681 0 None 33 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117170 10681 0 None 33 2 Human 7.8 pKi = 7.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340785 114305 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL334037 114305 0 None - 1 Human 6.8 pKi = 6.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11467328 86317 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 9 0 7 5.8 Cc1c(-c2ccc3oc4ccccc4c3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23198 86317 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 580 9 0 7 5.8 Cc1c(-c2ccc3oc4ccccc4c3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44346398 14369 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL120260 14369 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 638 10 0 8 6.8 CN(CCc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44346663 114317 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 592 10 0 9 5.2 COCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL334110 114317 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 592 10 0 9 5.2 COCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44451396 156132 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406958 156132 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 842 16 4 10 5.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047815 14779 0 None 30 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120834 14779 0 None 30 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11733484 186262 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 476 6 0 6 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)C)n3c2=O)c1 10.1021/jm0205402
CHEMBL48944 186262 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 476 6 0 6 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)C)n3c2=O)c1 10.1021/jm0205402
11168176 122506 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL360910 122506 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL73526 122506 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 397 7 1 6 2.5 COCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
10874838 100351 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 10 0 7 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL293247 100351 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 10 0 7 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
44435998 145762 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 522 6 0 6 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392087 145762 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 522 6 0 6 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
21047631 10858 0 None 5 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117330 10858 0 None 5 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44346848 112571 0 None 1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331204 112571 0 None 1 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
21045833 113192 0 None -11 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL332305 113192 0 None -11 2 Rat 5.8 pKi = 5.8 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncccn4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11318370 9610 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113151 9610 0 None - 1 Human 7.8 pKi = 7.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44394857 123839 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 7 1 7 5.4 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL363731 123839 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 7 1 7 5.4 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
44400204 167993 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 2 6 4.4 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL435689 167993 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 517 6 2 6 4.4 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44309390 167558 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)cc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL432922 167558 0 None - 1 Human 7.8 pKi = 7.8 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc(OC)cc4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44432628 87327 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL233762 87327 0 None - 1 Rat 7.8 pKi = 7.8 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 484 8 2 3 5.7 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)C2CCCC2)CC3)c1 10.1016/j.bmcl.2007.05.009
44387961 165468 0 None 144 2 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 165468 0 None 144 2 Human 7.8 pKi = 7.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44267864 167195 0 None 30 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
CHEMBL430312 167195 0 None 30 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
44267902 97952 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL275467 97952 0 None -6 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44287893 162654 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 919 11 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL418256 162654 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 919 11 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)CC3CC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267902 97952 0 None -6 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275467 97952 0 None -6 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44352665 117771 0 None 43 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL340934 117771 0 None 43 2 Human 6.8 pKi = 6.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11319703 122579 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 529 7 1 6 5.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1SC(F)(F)F 10.1021/jm049218c
CHEMBL361016 122579 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 529 7 1 6 5.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1SC(F)(F)F 10.1021/jm049218c
15462666 96055 4 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL262557 96055 4 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 624 9 0 8 6.7 CN(Cc1ccccc1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44435996 88357 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 9 0 7 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236342 88357 0 None - 1 Human 6.8 pKi = 6.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 9 0 7 4.0 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44387926 130093 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 528 8 1 8 3.2 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3Cl)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL368153 130093 0 None - 1 Human 6.8 pKi = 6.8 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 528 8 1 8 3.2 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3Cl)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
21047799 109914 0 None 6 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL324394 109914 0 None 6 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 559 9 2 5 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4c(C)noc4C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21048323 167149 0 None 8 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL430250 167149 0 None 8 2 Human 6.8 pKi = 6.8 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 421 5 1 2 6.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9851194 116184 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 578 10 0 8 5.6 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL337172 116184 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 578 10 0 8 5.6 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
44341057 162805 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL419212 162805 0 None - 1 Human 5.8 pKi = 5.8 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44435995 88301 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 524 9 0 6 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236137 88301 0 None - 1 Human 5.8 pKi = 5.8 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 524 9 0 6 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44340649 109147 0 None - 1 Human 4.8 pKi = 4.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL322283 109147 0 None - 1 Human 4.8 pKi = 4.8 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
11214294 121681 0 None -912 2 Rat 4.8 pKi = 4.8 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 121681 0 None -912 2 Rat 4.8 pKi = 4.8 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
11467134 123036 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm701249f
CHEMBL361798 123036 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm701249f
CHEMBL74686 123036 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm701249f
44400099 126904 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 509 8 1 7 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3SC)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL366020 126904 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 509 8 1 7 4.4 COc1cccc(-c2cn(Cc3c(F)cccc3SC)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
10962804 101325 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 566 9 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
CHEMBL300080 101325 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 566 9 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
44448991 154802 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL403234 154802 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL556355 154802 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 583 9 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44353246 20021 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 538 9 1 7 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130513 20021 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 538 9 1 7 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(N)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44340635 9598 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL113068 9598 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 471 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00619-x
44288078 156539 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 910 11 2 14 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL40743 156539 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 910 11 2 14 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL317064 209451 13 None - 1 Rat 5.7 pKi = 5.7 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
44451349 95705 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCNCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
CHEMBL260540 95705 0 None - 1 Human 5.7 pKi = 5.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCNCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.09.026
44434438 145662 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL392008 145662 0 None - 1 Human 6.7 pKi = 6.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1707 45 6 28 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44267875 15394 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12204 15394 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against human Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
10323198 123845 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL363759 123845 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
10323198 123845 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL363759 123845 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 487 6 1 6 4.7 Cc1c(-c2ccc(Cl)s2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44432657 148935 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394613 148935 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 635 10 3 3 7.2 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccc(C(=O)O)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
11671279 130362 0 None 331 2 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 130362 0 None 331 2 Human 8.7 pKi = 8.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44353262 116315 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL337919 116315 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
25156400 188272 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL506877 188272 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 581 12 2 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
21036877 173078 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL453441 173078 0 None - 1 Human 8.7 pKi = 8.7 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 627 13 2 7 5.9 Cc1c(-c2cccc(OCCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
44267876 97655 0 None 53 2 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273466 97655 0 None 53 2 Rat 8.7 pKi = 8.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 14 6.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11331001 188435 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL509075 188435 0 None - 1 Human 8.7 pKi = 8.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 12 2 7 5.2 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
1179 947 31 None 1 3 Mouse 8.7 pKi = 8.7 Binding
Binding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
9957278 947 31 None 1 3 Mouse 8.7 pKi = 8.7 Binding
Binding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL494803 947 31 None 1 3 Mouse 8.7 pKi = 8.7 Binding
Binding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to mouse gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL2371556 208337 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCCNC(=O)CCNC(=O)C[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371558 208339 0 None - 1 Rat 8.7 pKi = 8.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL439470 212093 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
11282957 121819 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
CHEMBL359894 121819 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
16058727 193151 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 548 7 1 7 4.6 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
CHEMBL539167 193151 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 548 7 1 7 4.6 COc1cccc(-c2nn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1Cl 10.1021/jm701249f
11282957 121819 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 121819 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
11282957 121819 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.01.009
CHEMBL359894 121819 0 None 1096 2 Human 8.6 pKi = 8.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.01.009
CHEMBL2371498 208315 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)C(C)(C)OC(C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)C(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
71459935 78548 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 466 7 1 4 4.5 COc1cccc(N2CN(Cc3c(F)cccc3F)C(=O)N(C[C@H](N)c3ccccc3)C2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL2113012 78548 0 None - 1 Human 8.6 pKi = 8.6 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 466 7 1 4 4.5 COc1cccc(N2CN(Cc3c(F)cccc3F)C(=O)N(C[C@H](N)c3ccccc3)C2=O)c1 10.1016/j.bmcl.2004.11.026
11466452 114238 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL333850 114238 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 515 8 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C3CCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL2371560 208341 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C)C(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL410819 211099 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@@H]2C(=O)NCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O)C(=O)O 10.1021/jm990115h
44347085 15083 0 None 3 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121145 15083 0 None 3 2 Rat 8.6 pKi = 8.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44400350 126475 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 6 1 5 5.5 Cc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c(Cl)c1 10.1016/j.bmcl.2005.03.057
CHEMBL365561 126475 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 6 1 5 5.5 Cc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c(Cl)c1 10.1016/j.bmcl.2005.03.057
44432641 166942 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL429976 166942 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 540 9 2 3 6.4 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2Cl)CC3)c1 10.1016/j.bmcl.2007.05.009
9831160 162918 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL419998 162918 0 None - 1 Human 8.6 pKi = 8.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
9831160 162918 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL419998 162918 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 665 15 1 8 7.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL385505 210606 0 None - 1 Rat 8.6 pKi = 8.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCCN)N(C(C)C)C(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3cccnc3)NC2=O)NC(=O)[C@@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11168311 165689 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL426783 165689 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
10077844 103308 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 637 13 1 8 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL308910 103308 0 None - 1 Human 8.6 pKi = 8.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 637 13 1 8 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
44267869 97668 0 None - 1 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)O[C@H](C)[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273535 97668 0 None - 1 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)O[C@H](C)[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44267902 97952 0 None 6 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275467 97952 0 None 6 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL405265 210805 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Affinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat Gonadotropin-releasing hormone receptor membrane evaluated using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCC(=O)NCC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
10919567 98573 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL280213 98573 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 664 10 1 7 7.4 CC(C)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
10347081 89080 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
CHEMBL23730 89080 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
11467134 123036 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm049218c
CHEMBL361798 123036 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm049218c
CHEMBL74686 123036 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1021/jm049218c
11272935 131265 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL369326 131265 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
CHEMBL75954 131265 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1021/jm049218c
44449186 95108 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL257599 95108 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
44394615 125364 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 572 7 1 8 5.1 Cc1c(-c2csc(-c3ccc4c(c3)CCO4)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL364840 125364 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 572 7 1 8 5.1 Cc1c(-c2csc(-c3ccc4c(c3)CCO4)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
10007333 9511 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112559 9511 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
10347081 89080 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23730 89080 0 None 223 2 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
10098618 110842 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL326804 110842 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11467134 123036 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL361798 123036 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL74686 123036 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1F 10.1016/j.bmcl.2004.02.004
44379092 157308 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1337 26 15 14 -0.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
CHEMBL408372 157308 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1337 26 15 14 -0.6 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44435975 91747 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 11 0 7 4.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL242399 91747 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 11 0 7 4.0 CCc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44436015 147038 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 8 0 7 4.6 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1Cc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL393092 147038 0 None - 1 Human 7.7 pKi = 7.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 591 8 0 7 4.6 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCN1Cc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44387907 60357 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 516 7 1 8 2.5 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL176056 60357 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 516 7 1 8 2.5 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)c3ccccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44387992 62196 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 496 7 1 8 2.7 COc1cccc(-n2c(=O)n(Cc3ccccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL178218 62196 0 None - 1 Human 7.7 pKi = 7.7 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 496 7 1 8 2.7 COc1cccc(-n2c(=O)n(Cc3ccccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21045797 170035 0 None 12 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL445074 170035 0 None 12 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL2371581 208349 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CCCCC1C[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)CNC(=O)CC[C@H](NC(C)=O)C(=O)N[C@H](Cc2ccc(Cl)cc2)C(=O)N1 10.1021/jm9901172
9984259 110012 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 110012 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
44343975 10477 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 586 11 0 8 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL116988 10477 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 586 11 0 8 5.3 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
11238637 67230 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 585 6 1 5 6.3 N[C@@H](Cn1c(=O)c(-c2ccc(C(F)(F)F)cc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL189964 67230 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 585 6 1 5 6.3 N[C@@H](Cn1c(=O)c(-c2ccc(C(F)(F)F)cc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11330280 122536 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL360934 122536 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL72606 122536 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 435 6 1 5 4.4 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CCCCC1 10.1016/j.bmcl.2004.02.004
9983568 98525 0 None 263 2 Human 6.7 pKi = 6.7 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 98525 0 None 263 2 Human 6.7 pKi = 6.7 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
9984259 110012 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Tested for binding affinity towards monkey gonadotropin releasing hormone receptorTested for binding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL324912 110012 0 None 281 2 Human 6.7 pKi = 6.7 Binding
Tested for binding affinity towards monkey gonadotropin releasing hormone receptorTested for binding affinity towards monkey gonadotropin releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
44352801 20143 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL130607 20143 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44340670 9550 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112730 9550 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL317341 209456 0 None - 1 Rat 5.7 pKi = 5.7 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc1c[nH]c2ccccc12)NC(C)=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
44287779 141042 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 979 12 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL384920 141042 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 979 12 2 14 7.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
21046762 10476 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116986 10476 0 None -9 2 Rat 5.7 pKi = 5.7 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44267885 17639 0 None -9 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12589 17639 0 None -9 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44267811 96767 0 None -14 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268491 96767 0 None -14 2 Human 5.7 pKi = 5.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 864 12 1 12 7.3 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44380024 168467 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1459 18 13 14 2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC1=O 10.1021/jm990116+
91931289 168467 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1459 18 13 14 2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC1=O 10.1021/jm990116+
CHEMBL439439 168467 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL 1459 18 13 14 2.4 CC(C)C[C@@H]1NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC1=O 10.1021/jm990116+
CHEMBL407855 210942 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H]1CC(=O)NC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
11490288 168082 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1021/jm049218c
CHEMBL436276 168082 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1021/jm049218c
CHEMBL75439 168082 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1021/jm049218c
44353304 18826 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 2 7 6.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL128810 18826 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 664 15 2 7 6.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL2371498 208315 0 None - 1 Rat 7.7 pKi = 7.7 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)C(C)(C)OC(C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)C(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
11354193 95767 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 640 9 1 8 3.8 COc1ccc(CN2CC3CC(c4ccc(N(C)C)c5ccccc45)N4C(=O)N(CCN5CCOCC5)C(=O)C34C2)cc1NC(C)=O 10.1016/j.bmc.2007.09.026
CHEMBL260816 95767 0 None - 1 Human 7.7 pKi = 7.7 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 640 9 1 8 3.8 COc1ccc(CN2CC3CC(c4ccc(N(C)C)c5ccccc45)N4C(=O)N(CCN5CCOCC5)C(=O)C34C2)cc1NC(C)=O 10.1016/j.bmc.2007.09.026
44340783 167336 0 None - 1 Human 6.7 pKi = 6.7 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL431248 167336 0 None - 1 Human 6.7 pKi = 6.7 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44394577 122706 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL361313 122706 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccccc1Nc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
44352513 117597 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 11 0 10 4.9 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCOC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL340677 117597 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 635 11 0 10 4.9 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCOC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
44340637 9488 0 None -1479 2 Rat 4.7 pKi = 4.7 Binding
Binding affinity towards rat GnRH gonadotropin releasing hormone receptorBinding affinity towards rat GnRH gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112466 9488 0 None -1479 2 Rat 4.7 pKi = 4.7 Binding
Binding affinity towards rat GnRH gonadotropin releasing hormone receptorBinding affinity towards rat GnRH gonadotropin releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44267874 96766 0 None -15 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL268489 96766 0 None -15 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 878 11 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
21047785 15285 0 None -20 2 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121576 15285 0 None -20 2 Rat 5.7 pKi = 5.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ccnc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44267885 17639 0 None 9 2 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12589 17639 0 None 9 2 Rat 6.7 pKi = 6.7 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 892 10 2 13 5.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCNC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11191153 193201 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL540207 193201 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
44576679 192835 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 12 2 7 4.3 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL526327 192835 0 None - 1 Human 7.7 pKi = 7.7 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 12 2 7 4.3 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
21047516 15173 0 None 1 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL121412 15173 0 None 1 2 Rat 7.7 pKi = 7.7 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
44267810 97640 0 None -5 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL273387 97640 0 None -5 2 Human 7.7 pKi = 7.7 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267810 97640 0 None -5 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273387 97640 0 None -5 2 Human 7.7 pKi = 7.7 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44577067 192634 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 5 1 6 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1021/jm701249f
CHEMBL523709 192634 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 477 5 1 6 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1021/jm701249f
11352630 88280 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 504 9 0 6 4.2 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL23604 88280 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 504 9 0 6 4.2 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
22716564 123273 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 5 1 6 4.4 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL362283 123273 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 477 5 1 6 4.4 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
10994908 162458 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 518 10 0 6 4.4 CCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL417558 162458 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 518 10 0 6 4.4 CCc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm034041s
44309321 202155 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
CHEMBL68625 202155 0 None - 1 Human 6.7 pKi = 6.7 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc(OC)cc2)nc2n(Cc3ccccc3F)c(C)c(-c3ccc4c(c3)OCO4)c(=O)n12 10.1016/s0960-894x(02)00371-2
21046762 10476 0 None 9 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116986 10476 0 None 9 2 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 464 5 3 3 4.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21047538 14389 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 555 8 3 6 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(F)c(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120397 14389 0 None - 1 Human 6.7 pKi = 6.7 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 555 8 3 6 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(F)c(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44390769 64540 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 486 6 1 7 2.5 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
CHEMBL182145 64540 0 None - 1 Human 6.7 pKi = 6.7 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 486 6 1 7 2.5 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
44309323 202350 0 None - 1 Human 5.7 pKi = 5.7 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 601 12 1 8 6.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN2CCCC2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL69914 202350 0 None - 1 Human 5.7 pKi = 5.7 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 601 12 1 8 6.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN2CCCC2)cc1 10.1016/s0960-894x(02)00370-0
44352735 117943 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 647 14 0 10 6.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL341124 117943 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 647 14 0 10 6.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11071561 101981 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 11 0 7 4.1 CCc1c(-c2cccc(OC)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL304002 101981 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 11 0 7 4.1 CCc1c(-c2cccc(OC)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44435820 160794 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 542 7 1 6 4.4 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(CCc2c[nH]c4ccccc24)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL412581 160794 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 542 7 1 6 4.4 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(CCc2c[nH]c4ccccc24)CC3)c1 10.1016/j.bmc.2007.05.029
44451460 155907 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)c2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406713 155907 0 None - 1 Human 5.7 pKi = 5.7 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)c2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11191675 63052 0 None -186 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 63052 0 None -186 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 63052 0 None -186 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
9958318 89796 0 None -15 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 89796 0 None -15 2 Rat 5.7 pKi = 5.7 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL266536 208942 0 None - 1 Rat 7.6 pKi = 7.6 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
44577051 186847 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 509 7 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)(N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL493794 186847 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 509 7 1 6 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)(N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44344157 110888 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 543 9 1 6 5.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL327076 110888 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 543 9 1 6 5.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](NC(C)C)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
44434404 166015 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL427981 166015 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1477 33 4 24 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44309582 202501 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 569 11 0 9 4.6 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00370-0
CHEMBL70851 202501 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 569 11 0 9 4.6 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00370-0
44389658 62916 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
CHEMBL179101 62916 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 459 5 1 6 4.2 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CS2)c1ccccc1 10.1021/jm701249f
12991507 186993 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 461 5 1 6 3.6 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1021/jm701249f
CHEMBL494621 186993 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 461 5 1 6 3.6 N[C@@H](Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1021/jm701249f
10940289 90217 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL23900 90217 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44312821 11958 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 409 8 1 5 4.0 CCCCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL1183624 11958 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 409 8 1 5 4.0 CCCCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL308154 11958 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 409 8 1 5 4.0 CCCCCn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
11330603 128156 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL366865 128156 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL430613 128156 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 459 7 1 6 3.9 COc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
22716524 123139 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 461 5 1 6 3.6 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL362025 123139 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 461 5 1 6 3.6 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1F)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
10940289 90217 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm034041s
CHEMBL23900 90217 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm034041s
44309525 102799 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 611 13 0 9 5.8 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00371-2
CHEMBL308446 102799 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 611 13 0 9 5.8 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00371-2
10557573 110959 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 870 22 9 8 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)N1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C1=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
CHEMBL327528 110959 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 870 22 9 8 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)N1C(=O)N[C@H](Cc2c[nH]c3ccccc23)C1=O)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
11671279 130362 0 None -331 2 Rat 5.6 pKi = 5.6 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 130362 0 None -331 2 Rat 5.6 pKi = 5.6 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44346848 112571 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331204 112571 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
10929667 85345 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22929 85345 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
10929667 85345 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL22929 85345 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44388002 121872 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CC[C@H](N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL360047 121872 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CC[C@H](N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047784 110148 0 None 36 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL325747 110148 0 None 36 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21046570 112588 0 None 34 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL331277 112588 0 None 34 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
11671279 130362 0 None 331 2 Human 7.6 pKi = 7.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL368511 130362 0 None 331 2 Human 7.6 pKi = 7.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 558 7 1 8 3.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Br)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
10929667 85345 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmc.2007.09.026
CHEMBL22929 85345 0 None - 1 Human 7.6 pKi = 7.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 548 9 0 8 3.7 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmc.2007.09.026
44340780 9657 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 543 13 0 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113455 9657 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 543 13 0 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)CCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
10929574 100665 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 538 8 1 6 6.3 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
CHEMBL295275 100665 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 538 8 1 6 6.3 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccc4)n3c2=O)c1 10.1021/jm0205402
11421243 90229 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2cccc(C(C)C)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23908 90229 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 10 0 6 5.0 Cc1c(-c2cccc(C(C)C)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
21048269 110608 0 None -2 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326313 110608 0 None -2 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 415 5 1 2 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccccc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11123821 201616 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 491 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccc3)c2=O)c1 10.1021/jm034041s
CHEMBL64795 201616 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 491 9 1 6 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccc3)c2=O)c1 10.1021/jm034041s
44387961 165468 0 None 144 2 Human 6.6 pKi = 6.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 165468 0 None 144 2 Human 6.6 pKi = 6.6 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44352548 168009 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cccc(F)c2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL435793 168009 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cccc(F)c2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44343932 168007 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 561 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL435784 168007 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 561 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
44436004 88318 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236197 88318 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44436005 88686 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCNC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236550 88686 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 508 6 1 6 3.5 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCNC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
10439527 168913 0 None 288 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL443027 168913 0 None 288 2 Human 7.6 pKi = 7.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11477970 89069 0 None 281 2 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 89069 0 None 281 2 Human 7.6 pKi = 7.6 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44436002 146563 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392731 146563 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44340784 9412 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112093 9412 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21045797 170035 0 None -12 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL445074 170035 0 None -12 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNC(=O)C(F)(F)F)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340804 9060 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccc(F)cc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL110052 9060 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccc(F)cc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
9825757 109669 0 None 12 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323687 109669 0 None 12 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340636 110753 0 None - 1 Human 5.6 pKi = 5.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL326510 110753 0 None - 1 Human 5.6 pKi = 5.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 415 6 1 6 2.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1 10.1016/s0960-894x(03)00620-6
44352514 18689 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 659 13 0 9 6.3 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C4CC4)C4CC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL128262 18689 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 659 13 0 9 6.3 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C4CC4)C4CC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
44309252 202137 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 589 9 0 7 5.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(Br)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68537 202137 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 589 9 0 7 5.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(Br)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44451385 95631 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 580 10 0 7 4.4 CC(C)CN(C)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(OC(F)(F)F)cc1)C2 10.1016/j.bmc.2007.09.026
CHEMBL260058 95631 0 None - 1 Human 5.6 pKi = 5.6 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 580 10 0 7 4.4 CC(C)CN(C)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(OC(F)(F)F)cc1)C2 10.1016/j.bmc.2007.09.026
11477970 89069 0 None -281 2 Rat 4.6 pKi = 4.6 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 89069 0 None -281 2 Rat 4.6 pKi = 4.6 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44267883 16137 0 None 3 2 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12265 16137 0 None 3 2 Rat 5.6 pKi = 5.6 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 780 9 2 11 5.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44435985 146417 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2007.05.029
CHEMBL392604 146417 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)c(Cl)c1)C2 10.1016/j.bmc.2007.05.029
44436008 88930 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.2 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(C5CCCC5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236965 88930 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.2 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(C5CCCC5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44435999 146565 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392733 146565 0 None - 1 Human 5.6 pKi = 5.6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 5.0 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4CC(C)C)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44394818 165566 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 530 7 1 7 5.1 Cc1c(-c2csc(-c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL426058 165566 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 530 7 1 7 5.1 Cc1c(-c2csc(-c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
21045828 14395 0 None 2 2 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120420 14395 0 None 2 2 Rat 7.6 pKi = 7.6 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44352515 116570 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 633 11 0 9 6.0 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL339211 116570 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 633 11 0 9 6.0 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
11766904 186059 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 561 11 0 7 5.7 CCN(CC)CCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL48806 186059 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 561 11 0 7 5.7 CCN(CC)CCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
44312666 11964 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 421 5 1 5 4.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL1183666 11964 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 421 5 1 5 4.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C1CCCCC1 10.1016/j.bmcl.2004.02.004
CHEMBL310716 11964 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 421 5 1 5 4.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1C1CCCCC1 10.1016/j.bmcl.2004.02.004
44451319 95728 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260647 95728 0 None - 1 Human 6.6 pKi = 6.6 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 882 15 3 10 6.0 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352874 22117 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 575 11 0 9 4.9 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL132387 22117 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 575 11 0 9 4.9 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44343976 10478 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 571 10 0 7 5.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL116989 10478 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 571 10 0 7 5.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3cccc(OC)c3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
11319401 121629 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL359681 121629 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 489 8 0 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
11261693 63078 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL179612 63078 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL74721 63078 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 463 6 1 5 4.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Cl 10.1016/j.bmcl.2004.02.004
44587399 188037 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 646 13 3 8 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL502967 188037 0 None - 1 Human 7.6 pKi = 7.6 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 646 13 3 8 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCNCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
44387908 62859 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 500 8 1 9 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3cccs3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL179023 62859 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 500 8 1 9 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3cccs3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
44287778 81168 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 15 2 14 7.8 CCC(C)N(CC1CC1)[C@H]1C[C@@H](C)OC(O[C@@H]2[C@@H](C)[C@H](OC3C[C@@](C)(OC)[C@@H](O)[C@H](C)O3)[C@@H](C)C(=O)O[C@H](CC)[C@@]3(C)OC(=O)N(CCc4ccc(Cl)cc4)[C@@H]3[C@@H](C)C(=O)[C@H](C)C[C@]2(C)OC)[C@@H]1O 10.1016/j.bmcl.2003.12.059
CHEMBL216252 81168 0 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 993 15 2 14 7.8 CCC(C)N(CC1CC1)[C@H]1C[C@@H](C)OC(O[C@@H]2[C@@H](C)[C@H](OC3C[C@@](C)(OC)[C@@H](O)[C@H](C)O3)[C@@H](C)C(=O)O[C@H](CC)[C@@]3(C)OC(=O)N(CCc4ccc(Cl)cc4)[C@@H]3[C@@H](C)C(=O)[C@H](C)C[C@]2(C)OC)[C@@H]1O 10.1016/j.bmcl.2003.12.059
44353264 22051 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 10 0 9 5.5 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(C3=NC(C)(C)CO3)c(=O)n12 10.1016/s0960-894x(01)00780-6
CHEMBL132339 22051 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 10 0 9 5.5 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(C3=NC(C)(C)CO3)c(=O)n12 10.1016/s0960-894x(01)00780-6
10050123 11078 0 None -20 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117863 11078 0 None -20 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 464 6 2 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(N)=O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44394852 126644 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 497 8 2 8 3.9 CCNc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
CHEMBL365695 126644 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 497 8 2 8 3.9 CCNc1nc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cs1 10.1016/j.bmcl.2004.07.022
44346374 113930 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL333233 113930 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 10 0 8 6.3 CCCCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
21045823 113643 0 None -40 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL332923 113643 0 None -40 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21046387 110163 0 None -53 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL325843 110163 0 None -53 2 Rat 5.6 pKi = 5.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
44267863 98066 0 None 2 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL276217 98066 0 None 2 2 Human 6.6 pKi = 6.6 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44387935 61770 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(CN)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL177523 61770 0 None - 1 Human 7.6 pKi = 7.6 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(CN)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
44347004 15275 0 None 13 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121535 15275 0 None 13 2 Human 7.6 pKi = 7.6 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44340798 108300 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL320920 108300 0 None - 1 Human 6.6 pKi = 6.6 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 505 9 1 6 4.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21047859 14048 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL119856 14048 0 None -1 2 Rat 6.6 pKi = 6.6 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44340644 9821 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 517 7 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(Cc4ccccc4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114399 9821 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 517 7 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(Cc4ccccc4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309399 202205 0 None - 1 Human 4.6 pKi = 4.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 518 10 1 7 5.4 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OC(CC)CC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL68964 202205 0 None - 1 Human 4.6 pKi = 4.6 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 518 10 1 7 5.4 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OC(CC)CC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
44352566 20458 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3cccnc3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL130861 20458 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3cccnc3)n2c1=O 10.1016/s0960-894x(01)00779-x
44309361 102262 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 7 0 9 4.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCOCC2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304950 102262 0 None - 1 Human 4.6 pKi = 4.6 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 582 7 0 9 4.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCOCC2)cc1 10.1016/s0960-894x(02)00371-2
44309585 202674 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 641 14 1 9 6.7 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccco2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL71793 202674 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 641 14 1 9 6.7 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccco2)cc1 10.1016/s0960-894x(02)00370-0
44587405 171674 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 673 13 2 7 6.6 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCC(C)(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL447424 171674 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 673 13 2 7 6.6 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCC(C)(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
44387918 60336 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 476 7 1 8 2.4 COc1cccc(-n2c(=O)n(Cc3ccccc3C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL176029 60336 0 None - 1 Human 7.5 pKi = 7.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 476 7 1 8 2.4 COc1cccc(-n2c(=O)n(Cc3ccccc3C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047519 14301 0 None 1 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
CHEMBL120048 14301 0 None 1 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
44434411 146220 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
CHEMBL392434 146220 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1521 36 4 25 9.5 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2nc(-c3ccc(NC(=O)NCc4cn(CCOCCOCCOCCn5cc(CNC(=O)Nc6ccc(-c7nc8n(Cc9c(F)cccc9F)cc(C(=O)OCC)c(=O)n8c7CN(C)Cc7ccccc7)cc6)nn5)nn4)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.04.065
44309375 103142 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 11 1 8 7.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2N2CCC3C=CC=CC3C2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL308696 103142 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 11 1 8 7.0 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2N2CCC3C=CC=CC3C2)cc1 10.1016/s0960-894x(02)00370-0
10345138 122042 0 None -2041 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 122042 0 None -2041 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 122042 0 None -2041 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
11226470 162519 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 538 10 0 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL417645 162519 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 538 10 0 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1F 10.1021/jm030472z
10027591 125750 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 467 6 1 6 4.4 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)s1 10.1016/j.bmcl.2004.07.022
CHEMBL365012 125750 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 467 6 1 6 4.4 Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)s1 10.1016/j.bmcl.2004.07.022
44387977 60196 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 548 7 1 8 3.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175711 60196 0 None - 1 Human 8.5 pKi = 8.5 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 548 7 1 8 3.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44347048 14344 0 None 18 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120164 14344 0 None 18 2 Rat 8.5 pKi = 8.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL438374 212019 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NCC(=O)NCC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
11375759 63504 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 5 4.5 Cc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL180262 63504 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 5 4.5 Cc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm049218c
11444886 122115 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1021/jm049218c
CHEMBL308289 122115 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1021/jm049218c
CHEMBL360367 122115 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1021/jm049218c
11467552 172142 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL450471 172142 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
11282957 121819 0 None 1096 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2008.04.029
CHEMBL359894 121819 0 None 1096 2 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2008.04.029
44576644 188388 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 7 5.0 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)C3CC3)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL508435 188388 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 7 5.0 N[C@@H](Cn1c(=O)c(-c2ccc(COC(=O)C3CC3)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353285 117231 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 678 17 2 7 7.1 CCCCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL340156 117231 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 678 17 2 7 7.1 CCCCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL2371585 208353 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@@H](C)C(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44378834 96380 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1291 24 12 15 -0.1 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
CHEMBL265169 96380 0 None - 1 Rat 8.5 pKi = 8.5 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1291 24 12 15 -0.1 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2cccnc2)NC1=O 10.1021/jm990115h
11455317 62559 0 None 851 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 62559 0 None 851 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
11467552 172142 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL450471 172142 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 603 11 2 6 5.7 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44576680 172969 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 627 13 2 9 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL453167 172969 0 None - 1 Human 8.5 pKi = 8.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 627 13 2 9 3.6 COc1cccc(-c2cn(Cc3c(F)cccc3S(C)(=O)=O)c(=O)n(C[C@H](NCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
11167850 2701 22 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 2701 22 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 2701 22 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 2701 22 None 6309 2 Human 8.5 pKi = 8.5 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
11191675 63052 0 None 186 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL179600 63052 0 None 186 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL3085404 63052 0 None 186 2 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm049218c
11456285 188347 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 613 12 2 8 4.1 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
CHEMBL508020 188347 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 613 12 2 8 4.1 CS(=O)(=O)c1cccc(F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](NCCCC(=O)O)c2ccccc2)c1=O 10.1016/j.bmcl.2008.04.036
44379006 168388 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1257 22 13 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)NCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](C)NC1=O 10.1021/jm990115h
CHEMBL438899 168388 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL 1257 22 13 15 -1.9 CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1cccnc1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CC(=O)NCC(=O)Nc2ccc(cc2)C[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](C)NC1=O 10.1021/jm990115h
11421518 164744 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
CHEMBL423291 164744 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
44449095 154971 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL404180 154971 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
25156942 188082 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](c3ccccc3)N(C)CCCC(=O)O)c2=O)c1F 10.1021/jm8006454
CHEMBL503705 188082 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](c3ccccc3)N(C)CCCC(=O)O)c2=O)c1F 10.1021/jm8006454
1179 947 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1021/jm701249f
9957278 947 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1021/jm701249f
CHEMBL494803 947 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity at rat GnRH receptor by competition binding assayBinding affinity at rat GnRH receptor by competition binding assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1021/jm701249f
44353258 115580 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 14 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL335647 115580 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 650 14 1 7 7.7 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(01)00780-6
1179 947 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
9957278 947 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL494803 947 31 None -1 3 Rat 8.4 pKi = 8.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to rat gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
44267868 97624 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL273275 97624 0 None -10 2 Human 8.4 pKi = 8.4 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
11421518 164744 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 164744 0 None 1047 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44388511 123150 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 515 6 1 5 5.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cc(F)ccc1C(F)(F)F 10.1021/jm049218c
CHEMBL362065 123150 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 515 6 1 5 5.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cc(F)ccc1C(F)(F)F 10.1021/jm049218c
9850211 187694 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL50009 187694 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 7 5.7 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
10886383 199223 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL60153 199223 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
44394901 66030 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccccc3Cl)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL185154 66030 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 564 7 1 7 5.8 Cc1c(-c2csc(-c3ccccc3Cl)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44400246 67314 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 569 9 1 8 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)C(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL190671 67314 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 569 9 1 8 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)C(C)C)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
10886383 199223 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL60153 199223 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 582 11 0 7 5.7 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44436003 88302 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236142 88302 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 619 9 0 7 5.0 O=c1c2c(n(Cc3c(F)cccc3F)c(=O)n1C[C@H]1CCCCN1CCc1ccccn1)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.05.029
44435980 146414 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(F)(F)F)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL392602 146414 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 10 0 7 4.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(F)(F)F)cc1)C2 10.1016/j.bmc.2007.05.029
11421518 164744 0 None 1047 2 Human 7.5 pKi = 7.5 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 164744 0 None 1047 2 Human 7.5 pKi = 7.5 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44309376 202406 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 600 13 1 9 5.4 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CC#N)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL70276 202406 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 600 13 1 9 5.4 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CC#N)cc1 10.1016/s0960-894x(02)00370-0
10929801 101467 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 564 11 0 9 4.2 COCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL301103 101467 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 564 11 0 9 4.2 COCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
44346349 113471 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 679 12 2 8 6.5 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL332616 113471 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 679 12 2 8 6.5 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44435976 88068 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 601 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(C)(C)C)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL235050 88068 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 601 10 0 7 4.8 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C(C)(C)C)cc1)C2 10.1016/j.bmc.2007.05.029
21047805 113951 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 588 10 2 7 7.0 COc1cc(OC)nc(NCC2CCC(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)CC2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL333349 113951 0 None - 1 Human 6.5 pKi = 6.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 588 10 2 7 7.0 COc1cc(OC)nc(NCC2CCC(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)CC2)n1 10.1016/s0960-894x(02)00756-4
11167850 2701 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1178 2701 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
1187 2701 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL179691 2701 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity at rat GnRH receptorBinding affinity at rat GnRH receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm701249f
11167850 2701 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1178 2701 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
1187 2701 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL179691 2701 22 None -6309 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for rat gonadotropin-releasing hormone receptorBinding affinity for rat gonadotropin-releasing hormone receptor
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm049218c
9825757 109669 0 None -12 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323687 109669 0 None -12 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 465 6 2 3 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](C(=O)O)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44394893 129148 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 469 6 2 8 3.1 Cc1c(-c2csc(N)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL367369 129148 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 469 6 2 8 3.1 Cc1c(-c2csc(N)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44451418 168152 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1620 32 9 19 8.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@H](C)NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436878 168152 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1620 32 9 19 8.2 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@H](C)NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44309522 96079 0 None - 1 Human 4.5 pKi = 4.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 476 8 1 7 4.3 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OCC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL262787 96079 0 None - 1 Human 4.5 pKi = 4.5 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 476 8 1 7 4.3 CCCC(=O)Nc1ccc(-c2cn3c(=O)c(C(=O)OCC)cn(Cc4ccccc4F)c3n2)cc1 10.1016/s0960-894x(02)00370-0
44435991 146422 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 8 4.7 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL392607 146422 0 None - 1 Human 6.5 pKi = 6.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 8 4.7 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44352652 116981 0 None 245 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL339968 116981 0 None 245 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL2371532 208328 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371584 208352 0 None - 1 Rat 7.5 pKi = 7.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44340825 167518 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL432585 167518 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44400255 134207 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 577 7 1 7 4.5 CS(=O)(=O)c1cccc(C(F)(F)F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
CHEMBL371855 134207 0 None - 1 Human 5.5 pKi = 5.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 577 7 1 7 4.5 CS(=O)(=O)c1cccc(C(F)(F)F)c1Cn1cc(-c2ccccc2Cl)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2005.03.057
44340808 110078 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL325326 110078 0 None - 1 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 532 8 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H]3CCCN3Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44593615 174049 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL455769 174049 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353200 20769 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 676 13 2 7 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL131127 20769 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 676 13 2 7 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
44593615 174049 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL455769 174049 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 12 1 8 5.3 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
10995320 187587 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 562 11 0 8 5.4 CCCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL49872 187587 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 562 11 0 8 5.4 CCCCN(C)Cc1c(C(C)(C)C(=O)OC)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
11785958 86611 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
CHEMBL23256 86611 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1021/jm030472z
11785958 86611 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23256 86611 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3OC)c2=O)c1 10.1016/s0960-894x(03)00619-x
44327851 110960 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 872 11 9 8 3.3 CC[C@H](C)[C@@H]1NC(=O)CSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O 10.1021/jm990432o
CHEMBL327529 110960 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL 872 11 9 8 3.3 CC[C@H](C)[C@@H]1NC(=O)CSC[C@@H](C(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O 10.1021/jm990432o
11180219 110733 0 None -112 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 110733 0 None -112 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
11226531 99059 0 None -169 2 Rat 5.5 pKi = 5.5 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 99059 0 None -169 2 Rat 5.5 pKi = 5.5 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
44451331 159334 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 8 1 6 4.8 NC(CC1CCCCC1)Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.09.026
CHEMBL410680 159334 0 None - 1 Human 5.5 pKi = 5.5 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 556 8 1 6 4.8 NC(CC1CCCCC1)Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2 10.1016/j.bmc.2007.09.026
21048462 109828 0 None -60 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323863 109828 0 None -60 2 Rat 5.5 pKi = 5.5 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44352657 21351 0 None 269 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
CHEMBL131665 21351 0 None 269 2 Human 7.5 pKi = 7.5 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
24857895 154781 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL403081 154781 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 551 8 1 6 5.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44394768 123864 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 605 10 2 10 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1OC 10.1016/j.bmcl.2004.07.022
CHEMBL363900 123864 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 605 10 2 10 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1OC 10.1016/j.bmcl.2004.07.022
11490288 168082 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL436276 168082 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1016/j.bmcl.2004.02.004
CHEMBL75439 168082 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1Cl 10.1016/j.bmcl.2004.02.004
44587392 169974 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 13 2 7 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL444989 169974 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 631 13 2 7 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
21045805 13672 0 None -5 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL119546 13672 0 None -5 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
21045829 112899 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331855 112899 0 None 1 2 Rat 7.5 pKi = 7.5 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44340771 9623 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113216 9623 0 None - 1 Human 6.5 pKi = 6.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 519 9 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44451398 168130 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1676 34 9 19 9.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H](NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)C(C)C)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436697 168130 0 None - 1 Human 5.5 pKi = 5.5 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1676 34 9 19 9.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H](NC(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)C(C)C)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
9958318 89796 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23830 89796 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44577096 178163 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 10 0 7 3.7 COc1cccc(-c2c(F)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL468546 178163 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 524 10 0 7 3.7 COc1cccc(-c2c(F)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
9958318 89796 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 89796 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
44394649 129650 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 1 8 5.2 Cc1c(-c2csc(N(C)c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL367812 129650 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 1 8 5.2 Cc1c(-c2csc(N(C)c3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
9958318 89796 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm049791w
CHEMBL23830 89796 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm049791w
9958318 89796 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23830 89796 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
9892420 201451 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL64148 201451 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity was determined towards human Gonadotropin-releasing hormone receptorBinding affinity was determined towards human Gonadotropin-releasing hormone receptor
ChEMBL 506 10 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3ccccn3)c2=O)c1 10.1021/jm034041s
44587391 171998 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.4 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL448656 171998 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 617 12 2 7 5.4 N[C@@H](Cn1c(=O)c(-c2cccc(OCCCCC(=O)O)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
9958318 89796 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL23830 89796 0 None 15 2 Human 7.5 pKi = 7.5 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.11.026
11352834 88761 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 516 10 0 6 4.5 C=Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL23673 88761 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 516 10 0 6 4.5 C=Cc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44394614 66608 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 9 2 8 5.1 Cc1c(-c2csc(NCc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL186646 66608 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 9 2 8 5.1 Cc1c(-c2csc(NCc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11272935 131265 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL369326 131265 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
CHEMBL75954 131265 0 None - 1 Human 7.5 pKi = 7.5 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 443 6 1 5 4.2 Cc1ccccc1Cn1c(C)c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c1=O 10.1016/j.bmcl.2004.02.004
44435829 88159 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
CHEMBL235520 88159 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)cc1 10.1016/j.bmc.2007.05.029
44587402 172136 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 674 14 2 8 5.1 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL450414 172136 0 None - 1 Human 7.5 pKi = 7.5 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 674 14 2 8 5.1 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
21047518 15276 0 None 10 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121551 15276 0 None 10 2 Human 7.5 pKi = 7.5 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11145953 183418 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 10 1 7 5.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CNCCc4ccccn4)cn3c2=O)c1 10.1021/jm0205402
CHEMBL48193 183418 0 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 539 10 1 7 5.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CNCCc4ccccn4)cn3c2=O)c1 10.1021/jm0205402
CHEMBL2371565 208342 0 None - 1 Rat 6.5 pKi = 6.5 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CC(=O)N[C@@H](C)C(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](CCCN=C(N)N)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44309576 101798 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 619 15 1 9 5.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCOC)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL303260 101798 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 619 15 1 9 5.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCOC)cc1 10.1016/s0960-894x(02)00370-0
10919052 113020 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL332138 113020 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 8 1 7 6.4 CN(Cc1ccccc1)Cc1c(-c2ccc(N)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44387988 131323 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 530 7 1 8 3.4 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL369453 131323 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 530 7 1 8 3.4 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44267866 96665 0 None -4 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL267568 96665 0 None -4 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44346260 114326 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 11 2 8 6.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL334148 114326 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 11 2 8 6.1 CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)CCN)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
11225384 127983 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
CHEMBL366701 127983 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm701249f
11225384 127983 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL366701 127983 0 None - 1 Human 7.4 pKi = 7.4 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2005.05.038
11225384 127983 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL366701 127983 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 480 7 1 8 2.2 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1016/j.bmcl.2004.11.026
11375912 84799 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 0 6 4.5 Cc1c(-c2cccc(Cl)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22559 84799 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 524 9 0 6 4.5 Cc1c(-c2cccc(Cl)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11260648 167474 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL432262 167474 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
11260648 167474 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL432262 167474 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309372 202165 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 677 13 0 10 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(OC)c(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL68698 202165 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 677 13 0 10 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cc(OC)c(OC)c(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44347004 15275 0 None -13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121535 15275 0 None -13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CNc4ccnc(NC[C@@H]5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44352933 21293 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL131589 21293 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44576657 187664 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 587 10 2 7 4.9 N[C@@H](Cn1c(=O)c(-c2ccc(CSCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499589 187664 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 587 10 2 7 4.9 N[C@@H](Cn1c(=O)c(-c2ccc(CSCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
11005990 89493 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23797 89493 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11005990 89493 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL23797 89493 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 534 9 0 8 3.6 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44587404 188453 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 661 14 2 8 5.2 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL509347 188453 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 661 14 2 8 5.2 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
44267868 97624 0 None -10 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273275 97624 0 None -10 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 933 10 1 14 7.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44435990 96059 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 585 10 0 8 5.2 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3CC3CCCCC3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL262580 96059 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 585 10 0 8 5.2 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3CC3CCCCC3)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
44451342 96018 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262334 96018 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 898 20 4 10 6.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047518 15276 0 None -10 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121551 15276 0 None -10 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 571 8 3 6 7.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4cc(Cl)nc(N)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44390795 121664 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 539 7 2 7 2.8 NC(Cc1c[nH]c2ccccc12)Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O 10.1016/j.bmcl.2004.11.026
CHEMBL359741 121664 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 539 7 2 7 2.8 NC(Cc1c[nH]c2ccccc12)Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2c(F)cccc2F)c1=O 10.1016/j.bmcl.2004.11.026
11113778 201432 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 495 10 2 7 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3c[nH]cn3)c2=O)c1 10.1021/jm034041s
CHEMBL64066 201432 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 495 10 2 7 2.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCCc3c[nH]cn3)c2=O)c1 10.1021/jm034041s
9891852 10000 0 None -23 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115482 10000 0 None -23 2 Rat 6.4 pKi = 6.4 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11178994 10304 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL116259 10304 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
11178994 10304 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL116259 10304 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
44593614 187679 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL499849 187679 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44593614 187679 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL499849 187679 0 None - 1 Human 5.4 pKi = 5.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 570 10 3 7 3.8 N[C@@H](Cn1c(=O)c(-c2ccc(CNCC(=O)O)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
11226531 99059 0 None 169 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 99059 0 None 169 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
44353228 19889 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 622 12 1 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130400 19889 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 622 12 1 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44400187 134760 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 551 6 1 5 5.6 N[C@@H](Cn1c(=O)c(-c2ccccc2C(F)(F)F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL372680 134760 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 551 6 1 5 5.6 N[C@@H](Cn1c(=O)c(-c2ccccc2C(F)(F)F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11444886 122115 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.02.004
CHEMBL308289 122115 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.02.004
CHEMBL360367 122115 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 497 6 1 5 4.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1C(F)(F)F 10.1016/j.bmcl.2004.02.004
10649568 14397 0 None -10 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
CHEMBL120432 14397 0 None -10 2 Rat 8.4 pKi = 8.4 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 517 7 3 6 4.9 Cc1cc(-c2c(OCC[C@@H]3CCN3)c3cc(C(=O)Nc4ccncn4)c(Cl)cc3[nH]c2=O)cc(C)c1C 10.1016/s0960-894x(03)00746-7
9983568 98525 0 None 263 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 98525 0 None 263 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
11283954 13982 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 8 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL119774 13982 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 529 8 0 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C3CCCCC3)N(C)C)c2=O)c1F 10.1021/jm049791w
44346667 113244 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL332355 113244 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 9 1 7 6.8 CC(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44587393 172065 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL449468 172065 0 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cellsDisplacement of [125I]Pro-N-Et-GnRH from human cloned GnRH receptor expressed in HEK cells
ChEMBL 613 12 2 7 5.5 Cc1c(-c2cccc(OCCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
10995569 101214 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccn1 10.1021/jm0205402
CHEMBL299348 101214 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccn1 10.1021/jm0205402
44449156 154505 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL401632 154505 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 565 9 1 6 5.7 CC[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL2371583 208351 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
CHEMBL2371479 208307 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H]1NC(=O)CC[C@@H]2NC(=O)[C@@H](NC(=O)[C@@H](Cc3cccnc3)NC(=O)[C@@H](Cc3ccc(Cl)cc3)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC(C)=O)CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCNC1=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC2=O 10.1021/jm990115h
25156944 188523 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 8 5.6 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/jm8006454
CHEMBL510285 188523 1 None - 1 Human 8.4 pKi = 8.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 12 1 8 5.6 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1021/jm8006454
44577098 177949 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 539 8 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3[S+](C)[O-])c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL466730 177949 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 539 8 1 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3[S+](C)[O-])c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44267810 97640 0 None 5 2 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273387 97640 0 None 5 2 Rat 8.4 pKi = 8.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 939 12 2 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11214614 188839 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1021/jm701249f
CHEMBL513346 188839 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1021/jm701249f
10051739 85008 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 85008 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
10051739 85008 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL22653 85008 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44449682 95600 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 533 8 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1 10.1016/j.bmcl.2008.04.029
CHEMBL259907 95600 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 533 8 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1 10.1016/j.bmcl.2008.04.029
10051739 85008 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL22653 85008 0 None 501 2 Human 8.4 pKi = 8.4 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm049791w
22716581 122008 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1016/j.bmcl.2005.01.009
CHEMBL360126 122008 0 None - 1 Human 8.4 pKi = 8.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 523 6 1 7 4.9 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1Cl 10.1016/j.bmcl.2005.01.009
44432638 86357 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232151 86357 0 None - 1 Rat 8.4 pKi = 8.4 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 506 9 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)Cc2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
11490509 63034 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 5 4.6 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Br 10.1021/jm049218c
CHEMBL179531 63034 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 5 4.6 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1Br 10.1021/jm049218c
9986320 100964 6 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human Gonadotropin-releasing hormone receptorBinding affinity to human Gonadotropin-releasing hormone receptor
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm0205402
CHEMBL297491 100964 6 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human Gonadotropin-releasing hormone receptorBinding affinity to human Gonadotropin-releasing hormone receptor
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm0205402
9986320 100964 6 None - 1 Human 8.3 pKi = 8.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL297491 100964 6 None - 1 Human 8.3 pKi = 8.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(OC)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL2371555 208336 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H]2CC(=O)N[C@H](C(=O)O)CNC(=O)[C@@H]3CCCN3C(=O)[C@@H]3CCCCNC(=O)CC[C@H](NC2=O)C(=O)N[C@H](Cc2ccc4ccccc4c2)C(=O)N[C@@H](CC(C)C)C(=O)N3)CCCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
10394119 113949 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards rat pituitary Gonadotropin-releasing hormone receptorBinding affinity towards rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 113949 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
Binding affinity towards rat pituitary Gonadotropin-releasing hormone receptorBinding affinity towards rat pituitary Gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44432646 146701 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL392843 146701 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 581 9 2 3 7.0 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCC2CCOCC2)CN(C(=O)Cc2ccccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44587395 172059 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 617 11 2 7 5.3 Cc1c(-c2cccc(OCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL449373 172059 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 617 11 2 7 5.3 Cc1c(-c2cccc(OCCCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
10394119 113949 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 113949 0 None 1 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9809382 100208 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL292291 100208 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 628 11 2 8 5.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL216633 207589 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CC(=O)NC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44449683 156771 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 9 2 7 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL407719 156771 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 517 9 2 7 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CO)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44577099 178165 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1021/jm701249f
CHEMBL468552 178165 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1021/jm701249f
9891852 95831 0 None 13 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL261145 95831 0 None 13 2 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
22716552 123253 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1016/j.bmcl.2005.01.009
CHEMBL362237 123253 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 507 6 1 7 4.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2F)CS3)c1F 10.1016/j.bmcl.2005.01.009
9891852 10953 0 None 18 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117736 10953 0 None 18 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9891852 95831 0 None 13 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL261145 95831 0 None 13 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21045829 112899 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331855 112899 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4nccc(NCC5CCCO5)n4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9891852 95831 0 None 13 2 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmc.2007.09.026
CHEMBL261145 95831 0 None 13 2 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/j.bmc.2007.09.026
44352607 20450 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 607 11 0 9 5.5 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
CHEMBL130855 20450 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 607 11 0 9 5.5 COc1ccc(-c2c(C#N)c3n(Cc4ccccc4F)cc(C(=O)OC(C)C)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00779-x
44352678 114735 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL334729 114735 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2ccc(F)cc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
10908122 183691 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1cccnc1 10.1021/jm0205402
CHEMBL48389 183691 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 597 10 0 9 5.1 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1cccnc1 10.1021/jm0205402
11027376 84805 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22563 84805 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11168330 98940 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
CHEMBL282707 98940 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
44353238 18351 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 553 10 0 7 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL127502 18351 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 553 10 0 7 5.8 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
11168330 98940 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL282707 98940 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
11027376 84805 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL22563 84805 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 490 9 0 6 3.9 Cc1c(-c2ccccc2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44451399 168155 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3cccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)c3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436906 168155 0 None - 1 Human 6.4 pKi = 6.4 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3cccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)c3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL2370259 208076 0 None - 1 Rat 5.4 pKi = 5.4 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None None 10.1021/jm990432o
44309357 97637 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 13 1 8 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
CHEMBL273358 97637 0 None - 1 Human 7.4 pKi = 7.4 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 651 13 1 8 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
44390780 63163 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 508 6 1 10 2.2 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccc3nsnc3c2)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
CHEMBL179953 63163 0 None - 1 Human 6.4 pKi = 6.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 508 6 1 10 2.2 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccc3nsnc3c2)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
11455317 62559 0 None 851 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 62559 0 None 851 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
44576681 192868 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 553 11 2 6 4.9 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL526887 192868 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 553 11 2 6 4.9 O=C(O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44353271 22368 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 10 1 7 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL132616 22368 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 580 10 1 7 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(C)=O)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44394767 125682 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL365001 125682 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 575 9 2 9 5.2 COc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
44394894 168303 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 548 7 1 7 5.3 Cc1c(-c2csc(-c3ccc(F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL438201 168303 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 548 7 1 7 5.3 Cc1c(-c2csc(-c3ccc(F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
9873729 11266 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 613 12 0 7 6.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL117977 11266 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 613 12 0 7 6.9 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00745-x
86276161 109365 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 441 6 1 7 4.8 COc1nc(F)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
CHEMBL3233520 109365 0 None - 1 Rat 7.4 pKi = 7.4 Binding
Displacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cellsDisplacement of [125I]Triptorelin from rat full-length gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 441 6 1 7 4.8 COc1nc(F)nc(OC)c1NC(=O)c1ccc(Oc2cc3c(cc2C)CCC3(C)C)o1 10.1016/j.bmcl.2014.02.002
21047858 9993 0 None 17 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115425 9993 0 None 17 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9828154 63538 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 523 10 0 9 2.1 COc1cccc(-n2c(=O)n(CCN(C)CCc3ccccn3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2004.11.026
CHEMBL180352 63538 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 523 10 0 9 2.1 COc1cccc(-n2c(=O)n(CCN(C)CCc3ccccn3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2004.11.026
44352747 21887 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 560 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL132179 21887 0 None - 1 Human 4.4 pKi = 4.4 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 560 10 0 8 5.5 CCOC(=O)c1cn(Cc2ccccc2)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00779-x
44267905 97912 0 None 13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275251 97912 0 None 13 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44346348 113855 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 8 6.1 C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL333103 113855 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 665 10 2 8 6.1 C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
11477988 90579 0 None 954 2 Human 7.4 pKi = 7.4 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 90579 0 None 954 2 Human 7.4 pKi = 7.4 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
11092567 101028 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 5.0 COCCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL297938 101028 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 5.0 COCCN(C)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
11103551 101208 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 544 8 1 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCCC4)n3c2=O)c1 10.1021/jm0205402
CHEMBL299320 101208 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 544 8 1 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCCC4)n3c2=O)c1 10.1021/jm0205402
44340632 9430 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112188 9430 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44312806 11216 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 433 6 1 6 3.8 Cc1ccc(Cn2c(C)c(-c3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)o1 10.1016/j.bmcl.2004.02.004
CHEMBL1179388 11216 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 433 6 1 6 3.8 Cc1ccc(Cn2c(C)c(-c3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)o1 10.1016/j.bmcl.2004.02.004
CHEMBL73454 11216 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 433 6 1 6 3.8 Cc1ccc(Cn2c(C)c(-c3ccccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)o1 10.1016/j.bmcl.2004.02.004
44353247 115561 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL335610 115561 0 None - 1 Human 7.4 pKi = 7.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
21047516 15173 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL121412 15173 0 None -1 2 Human 7.4 pKi = 7.4 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 595 12 3 7 6.9 COCCNc1nccc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
44353247 115561 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.09.026
CHEMBL335610 115561 0 None - 1 Human 7.4 pKi = 7.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 608 11 1 7 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)C(C)C)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/j.bmc.2007.09.026
44353265 22125 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 644 17 2 7 6.0 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCN(CC)CC)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL132392 22125 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 644 17 2 7 6.0 CCCCNC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(NC(=O)CCC)cc3)c(CN(C)CCN(CC)CC)n2c1=O 10.1016/s0960-894x(01)00780-6
21045834 16268 0 None -3 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL123301 16268 0 None -3 2 Rat 6.4 pKi = 6.4 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CNc4ncccn4)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11250647 1516 40 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
5293 1516 40 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
8362 1516 40 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
CHEMBL1208155 1516 40 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
DB11979 1516 40 None -117 2 Rat 5.4 pKi = 5.4 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 10.1021/jm8006454
44451406 96134 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 0 6 4.6 CC(CCN1CCc2c(c(=O)n(CCN3CCCCC3)c(=O)n2Cc2c(F)cccc2F)C1)CC(C)(C)C 10.1016/j.bmc.2007.09.026
CHEMBL263118 96134 0 None - 1 Human 5.4 pKi = 5.4 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 0 6 4.6 CC(CCN1CCc2c(c(=O)n(CCN3CCCCC3)c(=O)n2Cc2c(F)cccc2F)C1)CC(C)(C)C 10.1016/j.bmc.2007.09.026
11282957 121819 0 None 1096 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 121819 0 None 1096 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
44436018 146532 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 550 8 1 6 4.5 CN[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
CHEMBL392709 146532 0 None - 1 Human 7.4 pKi = 7.4 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 550 8 1 6 4.5 CN[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
44353305 19624 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 10 0 8 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc([N+](=O)[O-])cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL130195 19624 0 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 10 0 8 5.7 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc([N+](=O)[O-])cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL405918 210839 0 None - 1 Rat 6.4 pKi = 6.4 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CSSC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
11261195 63375 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL180124 63375 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
11261195 63375 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL180124 63375 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
11386605 89763 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23823 89763 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11786039 85354 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 540 9 0 6 5.0 Cc1c(-c2ccc3ccccc3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL22937 85354 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 540 9 0 6 5.0 Cc1c(-c2ccc3ccccc3c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
11386605 89763 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23823 89763 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccn3)c2=O)c1 10.1021/jm030472z
44346649 113067 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 589 7 1 9 4.5 O=c1c2c(CN3CCNCC3)c(-c3ccc([N+](=O)[O-])cc3)sc2n(Cc2c(F)cccc2F)c(=O)n1-c1ccccc1 10.1016/s0960-894x(03)00746-7
CHEMBL332194 113067 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 589 7 1 9 4.5 O=c1c2c(CN3CCNCC3)c(-c3ccc([N+](=O)[O-])cc3)sc2n(Cc2c(F)cccc2F)c(=O)n1-c1ccccc1 10.1016/s0960-894x(03)00746-7
44389571 62819 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 471 6 1 6 4.1 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2)CC3)c1F 10.1016/j.bmcl.2005.01.009
CHEMBL178961 62819 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 471 6 1 6 4.1 COc1cccc(-c2c3n(c(=O)n(C[C@H](N)c4ccccc4)c2=O)C(c2ccccc2)CC3)c1F 10.1016/j.bmcl.2005.01.009
44267903 161683 0 None -3 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL416337 161683 0 None -3 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 906 10 1 13 6.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCN(C)C2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44394779 66733 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3ccc(C(F)(F)F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL187243 66733 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 598 7 1 7 6.2 Cc1c(-c2csc(-c3ccc(C(F)(F)F)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
44309559 102489 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL306431 102489 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00371-2
44309559 102489 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.09.026
CHEMBL306431 102489 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 616 9 0 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/j.bmc.2007.09.026
44340656 109988 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL324759 109988 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44340652 9364 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL111820 9364 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
11238459 89110 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 570 9 0 8 4.2 Cc1c(-c2ccc3c(c2)OC(F)(F)O3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL23737 89110 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 570 9 0 8 4.2 Cc1c(-c2ccc3c(c2)OC(F)(F)O3)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44432645 86774 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL232752 86774 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 487 5 2 2 5.6 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CN)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44267906 166931 0 None -9 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL429949 166931 0 None -9 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
10983989 199988 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 9 1 7 3.6 Cc1c(-c2cccc(O)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL60618 199988 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 506 9 1 7 3.6 Cc1c(-c2cccc(O)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44451276 95595 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL259878 95595 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11284264 84331 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 550 11 0 8 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1OC 10.1021/jm030472z
CHEMBL22300 84331 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 550 11 0 8 3.9 COc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1OC 10.1021/jm030472z
10907714 201471 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL64212 201471 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 546 9 0 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCC[C@@H]3Cc3ccccn3)c2=O)c1 10.1021/jm034041s
11124671 201494 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 574 10 0 7 4.8 Cc1c(-c2cccc(OC(F)(F)F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
CHEMBL64273 201494 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 574 10 0 7 4.8 Cc1c(-c2cccc(OC(F)(F)F)c2)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm034041s
44394608 66728 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL187217 66728 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 559 8 2 8 5.5 Cc1ccc(Nc2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
44394841 165409 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 562 7 1 7 5.6 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1F 10.1016/j.bmcl.2004.07.022
CHEMBL425178 165409 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 562 7 1 7 5.6 Cc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1F 10.1016/j.bmcl.2004.07.022
CHEMBL412504 211252 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@H]1CC(=O)NCC(=O)NC[C@@H]2NC(=O)[C@H](Cc3ccc(O)cc3)NC(=O)[C@H](CC(=O)NC[C@@H](C(N)=O)NC(=O)[C@@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC1=O 10.1021/jm990116+
11124921 191204 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 612 10 1 9 5.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1O 10.1021/jm0205402
CHEMBL51983 191204 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 612 10 1 9 5.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1O 10.1021/jm0205402
44436010 88932 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 4.8 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL236967 88932 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 599 8 0 7 4.8 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(Cc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44352957 116232 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 600 11 0 10 4.8 CCOC(=O)c1cn(Cc2ccccc2C#N)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL337433 116232 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 600 11 0 10 4.8 CCOC(=O)c1cn(Cc2ccccc2C#N)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11214860 84347 0 None -323 2 Rat 5.3 pKi = 5.3 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
CHEMBL22314 84347 0 None -323 2 Rat 5.3 pKi = 5.3 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 541 10 1 7 4.8 CCc1ccc(CN[C@@H](C)Cn2c(=O)c(-c3cccc(OC)c3F)c(C)n(Cc3c(F)cccc3F)c2=O)o1 10.1021/jm030472z
11191675 63052 0 None 186 2 Human 8.3 pKi = 8.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 63052 0 None 186 2 Human 8.3 pKi = 8.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 63052 0 None 186 2 Human 8.3 pKi = 8.3 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
44340637 9488 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.07.022
CHEMBL112466 9488 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2004.07.022
44340652 9364 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL111820 9364 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00619-x
17757566 88114 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 10 0 7 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL235270 88114 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 573 10 0 7 4.1 Cc1ccc(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
17757565 146421 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 593 10 0 7 4.4 Cc1cc(Cl)ccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
CHEMBL392605 146421 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 593 10 0 7 4.4 Cc1cc(Cl)ccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
44387972 63545 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 514 7 1 8 2.8 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL180372 63545 0 None - 1 Human 8.3 pKi = 8.3 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 514 7 1 8 2.8 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
11214294 121681 0 None 912 2 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 121681 0 None 912 2 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
44340749 108631 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL321376 108631 0 None - 1 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
9829468 188181 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL50546 188181 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44340749 108631 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL321376 108631 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1021/jm701249f
9829468 188181 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm701249f
CHEMBL50546 188181 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 567 9 0 7 6.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)CCc4ccccn4)n3c2=O)c1 10.1021/jm701249f
CHEMBL2371542 208334 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293Competitive radioligand binding assay for rat Gonadotropin-releasing hormone receptor cells stably transfected in human HEK293
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)N[C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc2ccc(O)cc2)C(=O)N[C@H](Cc2ccc3ccccc3c2)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)CCCNC(=O)[C@@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm9901172
44434414 88098 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
CHEMBL235179 88098 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 709 14 3 9 4.6 C#CCNC(=O)CN(Cc1ccccc1)Cc1c(-c2ccc(NC(=O)NCC)cc2)nc2n(Cc3c(F)cccc3F)cc(C(=O)OCC)c(=O)n12 10.1016/j.bmc.2007.04.065
44267906 166931 0 None 9 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL429949 166931 0 None 9 2 Rat 8.3 pKi = 8.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44399944 68293 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL191817 68293 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44399944 68293 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
44399944 68293 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
CHEMBL191817 68293 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL191817 68293 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2008.04.036
44399944 68293 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL191817 68293 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44340637 9488 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112466 9488 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44340637 9488 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1021/jm701249f
CHEMBL112466 9488 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1021/jm701249f
44340637 9488 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2005.01.009
CHEMBL112466 9488 0 None 1479 2 Human 8.3 pKi = 8.3 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 520 9 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N(C)Cc3ccccn3)c2=O)c1 10.1016/j.bmcl.2005.01.009
11156980 62264 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL178281 62264 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 505 7 1 7 4.0 CN[C@@H](Cn1c(=O)c(-c2ccc3c(c2)OCO3)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
11374717 121781 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359810 121781 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL419270 121781 0 None - 1 Human 8.3 pKi = 8.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
44399944 68293 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL191817 68293 0 None - 1 Human 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44432639 86535 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
CHEMBL232356 86535 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 536 10 2 4 5.8 COc1ccccc1CC(=O)N1CCc2[nH]c(-c3cc(C)cc(C)c3)c([C@H](C)CNCCc3ccncc3)c2C1 10.1016/j.bmcl.2007.05.009
44267887 98029 0 None -41 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275935 98029 0 None -41 3 Human 8.3 pKi = 8.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 967 10 1 14 7.8 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL414275 211371 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CSSC[C@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc3ccc4ccccc4c3)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44353249 167881 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 659 17 1 8 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCN(CC)CC)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL434995 167881 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 659 17 1 8 6.8 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCN(CC)CC)cc1 10.1016/s0960-894x(01)00780-6
10051739 85008 0 None 501 2 Human 7.3 pKi = 7.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 85008 0 None 501 2 Human 7.3 pKi = 7.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
44451350 95709 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 544 8 1 6 4.5 CNC(Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C)cc1C)C2)c1ccccc1 10.1016/j.bmc.2007.09.026
CHEMBL260552 95709 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 544 8 1 6 4.5 CNC(Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(C)cc1C)C2)c1ccccc1 10.1016/j.bmc.2007.09.026
9939030 155187 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 623 11 1 6 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2cc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)cc2c1=O 10.1016/j.bmc.2007.09.026
CHEMBL405449 155187 0 None - 1 Human 7.3 pKi = 7.3 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 623 11 1 6 7.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2cc(-c3ccc(NC(=O)CC)cc3)c(CN(C)Cc3ccccc3)cc2c1=O 10.1016/j.bmc.2007.09.026
44267882 166031 0 None 12 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL428008 166031 0 None 12 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
14557580 88940 0 None - 1 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 972 26 11 11 0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cccc2ccccc12 10.1021/jm00130a019
CHEMBL2369785 88940 0 None - 1 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constantIn vitro binding affinity towards luteinizing hormone receptor from rat pituitary cells is expressed as negative logarithm of the equilibrium dissociation constant
ChEMBL 972 26 11 11 0.3 CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cccc2ccccc12 10.1021/jm00130a019
9916573 156513 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 593 11 0 9 5.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL407399 156513 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 593 11 0 9 5.1 CCOC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44394578 129649 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 586 7 1 7 6.4 Cc1c(-c2csc(-c3ccc(C(C)(C)C)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL367806 129649 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 586 7 1 7 6.4 Cc1c(-c2csc(-c3ccc(C(C)(C)C)cc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11752557 63368 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1016/j.bmcl.2004.02.004
CHEMBL180117 63368 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1016/j.bmcl.2004.02.004
CHEMBL74925 63368 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1016/j.bmcl.2004.02.004
44451498 155081 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1700 30 7 19 9.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC(C(=O)NCC#Cc3ccccc3C#CCNC(=O)C3CCN(C(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)CC3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL404611 155081 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1700 30 7 19 9.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC(C(=O)NCC#Cc3ccccc3C#CCNC(=O)C3CCN(C(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)CC3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL2370249 208070 0 None - 1 Rat 6.3 pKi = 6.3 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]cn1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
11202795 112335 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL330804 112335 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
11477970 89069 0 None 281 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL23729 89069 0 None 281 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm049791w
11202795 112335 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL330804 112335 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
21046387 110163 0 None 53 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL325843 110163 0 None 53 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 493 7 1 4 6.6 CCOC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
44267875 15394 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL12204 15394 0 None - 1 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity was determined against rat Luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 879 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44451391 168298 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)cc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL438168 168298 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1715 30 6 20 10.7 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC(C(=O)NCC#Cc3ccc(C#CCNC(=O)C4CCN(C(=O)CN(Cc5ccccc5)Cc5c(-c6ccc(NC(=O)NCC)cc6)nc6n(Cc7c(F)cccc7F)cc(C(=O)OCC)c(=O)n56)CC4)cc3)CC2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21046569 11903 0 None - 1 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 9 2 7 7.0 COC(=O)c1cc(C)nc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
CHEMBL118330 11903 0 None - 1 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 594 9 2 7 7.0 COC(=O)c1cc(C)nc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)n1 10.1016/s0960-894x(02)00756-4
21045818 112597 0 None -3 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331337 112597 0 None -3 2 Rat 6.3 pKi = 6.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 522 8 2 5 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncccn4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11050500 101378 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 636 9 0 8 6.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCC(c2ccccc2)CC1 10.1021/jm0205402
CHEMBL300484 101378 0 None - 1 Human 5.3 pKi = 5.3 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 636 9 0 8 6.5 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCC(c2ccccc2)CC1 10.1021/jm0205402
44435828 88677 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 11 1 7 4.0 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(CCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2007.05.029
CHEMBL236546 88677 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 11 1 7 4.0 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(CCc1c[nH]c3ccccc13)C2 10.1016/j.bmc.2007.05.029
44309631 102136 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 652 14 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2cccnc2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL304156 102136 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 652 14 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)Cc2cccnc2)cc1 10.1016/s0960-894x(02)00370-0
44587397 171787 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 589 9 2 7 4.5 Cc1c(-c2cccc(OCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL447592 171787 0 None - 1 Human 7.3 pKi = 7.3 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 589 9 2 7 4.5 Cc1c(-c2cccc(OCC(=O)O)c2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
9891852 95831 0 None -13 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL261145 95831 0 None -13 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 4 3 5.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44436000 146669 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.3 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C4CCCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL392815 146669 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 576 7 0 6 5.3 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4C4CCCC4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
21045831 10395 0 None -7 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116611 10395 0 None -7 2 Rat 5.3 pKi = 5.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
21047815 14779 0 None -30 2 Rat 5.3 pKi = 5.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120834 14779 0 None -30 2 Rat 5.3 pKi = 5.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 562 8 2 5 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(Cl)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44340646 9597 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL113059 9597 0 None - 1 Human 7.3 pKi = 7.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11421385 167857 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1021/jm049218c
CHEMBL433302 167857 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1021/jm049218c
CHEMBL434906 167857 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1021/jm049218c
11049737 101892 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 532 8 0 7 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCCC3c3ccccn3)c2=O)c1 10.1021/jm034041s
CHEMBL303811 101892 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptorBinding affinity was determined towards human gonadotropin-releasing hormone receptor
ChEMBL 532 8 0 7 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN3CCCC3c3ccccn3)c2=O)c1 10.1021/jm034041s
44451345 96063 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262599 96063 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1607 32 8 20 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCC(=O)NCC#Cc2ccc(C#CCNC(=O)CNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44451474 168192 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL437260 168192 0 None - 1 Human 5.3 pKi = 5.3 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1635 32 8 20 9.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@@H](C)C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@H](C)NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21048462 109828 0 None 60 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL323863 109828 0 None 60 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 522 5 1 4 6.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCN(C(=O)OC(C)(C)C)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44433200 149651 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 555 7 0 8 4.1 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccc(-n4ccnc4)cc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL395183 149651 0 None - 1 Human 6.3 pKi = 6.3 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 555 7 0 8 4.1 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccc(-n4ccnc4)cc2)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL415608 211447 0 None - 1 Rat 7.3 pKi = 7.3 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44343931 109912 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL324375 109912 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00780-6
9910626 10290 0 None 1 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
CHEMBL116246 10290 0 None 1 2 Rat 7.3 pKi = 7.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
44343931 109912 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL324375 109912 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 568 11 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
44400195 69045 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL193089 69045 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 531 7 1 6 4.7 COc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
21047519 14301 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
CHEMBL120048 14301 0 None -1 2 Rat 7.3 pKi = 7.3 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 551 8 3 6 6.8 Cc1cc(NCc2cccc(CNC(=O)c3ccc(Cc4cc5c(cc4C)C(C)(C)CCC5(C)C)o3)c2)nc(N)n1 10.1016/s0960-894x(02)00756-4
44340697 110180 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL325942 110180 0 None - 1 Human 6.3 pKi = 6.3 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 492 9 1 7 3.5 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCNCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
44340612 9487 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112461 9487 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
11477970 89069 0 None 281 2 Human 6.3 pKi = 6.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
CHEMBL23729 89069 0 None 281 2 Human 6.3 pKi = 6.3 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3ccccc3)c2=O)c1F 10.1021/jm030472z
44309359 101856 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 619 10 1 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(S)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL303621 101856 0 None - 1 Human 7.3 pKi = 7.3 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 619 10 1 8 6.7 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(S)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
9910626 10290 0 None -1 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
CHEMBL116246 10290 0 None -1 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 431 5 1 4 5.6 Cc1cnc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cn1 10.1016/s0960-894x(02)00755-2
44347048 14344 0 None -18 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120164 14344 0 None -18 2 Human 7.3 pKi = 7.3 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9911446 10681 0 None -33 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117170 10681 0 None -33 2 Rat 6.3 pKi = 6.3 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 446 5 1 3 6.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(C#N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44267864 167195 0 None -30 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
CHEMBL430312 167195 0 None -30 2 Human 6.3 pKi = 6.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CCC1CN(C(=O)O[C@H]2[C@H](C)[C@@H](OC3O[C@H](C)C[C@H](N(C)C(C)C)[C@H]3O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]3N(CCc4ccc(Cl)cc4)C(=O)O[C@]3(C)[C@@H](CC)OC(=O)[C@@H]2C)C(=O)O1 10.1021/jm030418i
44267905 97912 0 None -13 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275251 97912 0 None -13 2 Human 5.3 pKi = 5.3 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11421385 167857 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL433302 167857 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1016/j.bmcl.2004.02.004
CHEMBL434906 167857 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 429 6 1 5 3.9 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccc1 10.1016/j.bmcl.2004.02.004
44347005 113966 0 None -6 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333461 113966 0 None -6 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11752557 63368 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1021/jm049218c
CHEMBL180117 63368 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1021/jm049218c
CHEMBL74925 63368 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 395 6 1 5 3.5 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC(C)C 10.1021/jm049218c
44399956 123527 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL363094 123527 1 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 481 7 1 6 3.9 COc1cccc(-c2cn(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44346239 14342 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 707 12 2 8 7.2 CC(C)C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL120149 14342 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 707 12 2 8 7.2 CC(C)C[C@H](N)C(=O)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
44434436 150440 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395825 150440 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1619 39 6 26 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44577100 177917 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 452 6 1 6 3.1 N[C@@H](Cn1c(=O)c(Cc2c(F)cccc2F)nn(-c2ccccc2F)c1=O)c1ccccc1 10.1021/jm701249f
CHEMBL466541 177917 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 452 6 1 6 3.1 N[C@@H](Cn1c(=O)c(Cc2c(F)cccc2F)nn(-c2ccccc2F)c1=O)c1ccccc1 10.1021/jm701249f
44451356 95916 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL261649 95916 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 870 18 4 10 5.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44387909 122252 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 495 8 1 9 2.0 COc1cccc(-n2c(=O)n(CCC(N)c3cccnc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL360472 122252 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 495 8 1 9 2.0 COc1cccc(-n2c(=O)n(CCC(N)c3cccnc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
9960268 188400 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 596 10 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1 10.1021/jm0205402
CHEMBL50856 188400 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 596 10 0 8 5.8 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN(C)Cc1ccccc1 10.1021/jm0205402
44340844 110064 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL325233 110064 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11751752 13451 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049791w
CHEMBL119391 13451 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049791w
11374717 121781 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL359810 121781 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
CHEMBL419270 121781 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm701249f
44400230 68342 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL192172 68342 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
1179 947 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
9957278 947 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
CHEMBL494803 947 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Binding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assayBinding affinity to human gonadotropin-releasing hormone receptor by radioligand displacement assay
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1016/j.bmcl.2014.02.002
44400230 68342 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL192172 68342 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 1 5 4.4 N[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11374717 121781 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL359810 121781 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.02.004
CHEMBL419270 121781 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 465 6 1 5 4.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.02.004
1179 947 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Displacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
9957278 947 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Displacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
CHEMBL494803 947 31 None -4 3 Human 8.2 pKi = 8.2 Binding
Displacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting methodDisplacement of lzsI-GnRH-A from human GnRHR expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method
ChEMBL 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1039/C7MD00320J
21045805 13672 0 None 5 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL119546 13672 0 None 5 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44215933 95632 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3nccs3)c2=O)c1F 10.1016/j.bmc.2007.09.026
CHEMBL260062 95632 0 None - 1 Human 8.2 pKi = 8.2 Binding
Inhibition of GnRH receptorInhibition of GnRH receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCc3nccs3)c2=O)c1F 10.1016/j.bmc.2007.09.026
44432655 148954 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL394634 148954 0 None - 1 Rat 8.2 pKi = 8.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 675 11 3 6 6.5 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCOc2ccc(-c4nnn[nH]4)cc2)CN(C(=O)Cc2c(F)cccc2C(F)(F)F)CC3)c1 10.1016/j.bmcl.2007.05.009
44400354 132983 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 559 8 1 6 5.5 CC(C)Oc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL370711 132983 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 559 8 1 6 5.5 CC(C)Oc1cccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44267865 160837 0 None 10 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
CHEMBL412634 160837 0 None 10 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
11236870 10943 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL117670 10943 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049218c
11294792 62958 0 None 380 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 62958 0 None 380 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
10345138 122042 0 None 2041 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL360143 122042 0 None 2041 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
CHEMBL75347 122042 0 None 2041 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 481 6 1 5 4.7 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1Cl 10.1021/jm049218c
11236870 10943 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL117670 10943 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 475 8 1 6 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)C)c2=O)c1F 10.1021/jm049791w
11226753 63014 0 None 389 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL179429 63014 0 None 389 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 8 0 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](c3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11180219 110733 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
CHEMBL326504 110733 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049218c
11180219 110733 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL326504 110733 0 None 112 2 Human 8.2 pKi = 8.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 501 7 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)C3CCCCC3)c2=O)c1F 10.1021/jm049791w
9823968 109992 0 None 1 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
CHEMBL324771 109992 0 None 1 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
1184 3676 31 None -426 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
9874838 3676 31 None -426 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
CHEMBL71917 3676 31 None -426 2 Rat 7.2 pKi = 7.2 Binding
Binding affinity towards rat Gonadotropin-releasing hormone receptorBinding affinity towards rat Gonadotropin-releasing hormone receptor
ChEMBL 657 11 1 7 7.8 CC(OC(=O)c1cn(Cc2c(F)cccc2F)c2c(c1=O)c(CN(Cc1ccccc1)C)c(s2)c1ccc(cc1)NC(=O)C(C)C)C 10.1016/s0960-894x(03)00746-7
11751752 13451 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049218c
CHEMBL119391 13451 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 433 6 1 6 2.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)N)c2=O)c1F 10.1021/jm049218c
44436011 88067 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 9 0 7 4.9 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(CCc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL235046 88067 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 613 9 0 7 4.9 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCN(CCc5ccccn5)C4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44451447 156133 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406960 156133 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352949 115581 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL335650 115581 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 611 11 0 9 5.2 CCOC(=O)c1cn(Cc2cc(F)ccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11444384 63089 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1021/jm049218c
CHEMBL179663 63089 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1021/jm049218c
CHEMBL311380 63089 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1021/jm049218c
44449120 94789 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
CHEMBL256109 94789 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 567 8 1 6 5.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1Cl 10.1016/j.bmcl.2008.04.029
44346666 112340 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 9 0 7 6.9 CN(Cc1ccccc1)Cc1c(-c2ccc(N(C)C)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL330835 112340 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 622 9 0 7 6.9 CN(Cc1ccccc1)Cc1c(-c2ccc(N(C)C)cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
9958318 89796 0 None 15 2 Human 6.2 pKi = 6.2 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23830 89796 0 None 15 2 Human 6.2 pKi = 6.2 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 520 10 0 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)c1 10.1021/jm030472z
11167850 2701 22 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1178 2701 22 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
1187 2701 22 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL179691 2701 22 None -6309 2 Rat 5.2 pKi = 5.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
ChEMBL 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 10.1021/jm8006454
CHEMBL216930 207601 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44353231 116309 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 595 12 0 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
CHEMBL337865 116309 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 595 12 0 7 6.9 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2cc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(01)00780-6
44451420 95766 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260812 95766 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44387883 62944 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 478 8 1 8 2.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)CC(C)C)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL179212 62944 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 478 8 1 8 2.0 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(CC(N)CC(C)C)c2=O)c1F 10.1016/j.bmcl.2005.05.038
11341990 62171 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1021/jm049218c
CHEMBL178127 62171 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1021/jm049218c
CHEMBL76277 62171 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1021/jm049218c
21047807 112487 0 None 23 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL331087 112487 0 None 23 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 568 8 3 7 6.4 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4ncc(C#N)c(N)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44353284 167824 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 652 15 2 8 5.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCOC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL434621 167824 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 652 15 2 8 5.1 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NCCOC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
44388009 128162 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 7 1 8 2.9 COc1cccc(-n2c(=O)n(C[C@H](N)c3ccccc3)c(=O)n(C(C)c3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL366883 128162 0 None - 1 Human 6.2 pKi = 6.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 7 1 8 2.9 COc1cccc(-n2c(=O)n(C[C@H](N)c3ccccc3)c(=O)n(C(C)c3c(F)cccc3F)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44267882 166031 0 None -12 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL428008 166031 0 None -12 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 876 11 1 12 7.4 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)C2CCCC2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11238091 62177 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1021/jm049218c
CHEMBL178142 62177 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1021/jm049218c
CHEMBL311407 62177 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1021/jm049218c
44353263 22048 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 634 10 0 9 6.9 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(-c3nc(C(C)(C)C)co3)c(=O)n12 10.1016/s0960-894x(01)00780-6
CHEMBL132338 22048 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 634 10 0 9 6.9 CN(CCc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)cc2n(Cc3ccccc3F)cc(-c3nc(C(C)(C)C)co3)c(=O)n12 10.1016/s0960-894x(01)00780-6
44346594 15398 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 548 7 0 8 5.2 CN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL122064 15398 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 548 7 0 8 5.2 CN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44295109 101211 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 530 8 1 6 6.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCC4)n3c2=O)c1 10.1021/jm0205402
CHEMBL299335 101211 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 530 8 1 6 6.2 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CNCC4CCCC4)n3c2=O)c1 10.1021/jm0205402
11477988 90579 0 None -954 2 Rat 5.2 pKi = 5.2 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
CHEMBL23969 90579 0 None -954 2 Rat 5.2 pKi = 5.2 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 524 9 1 7 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3ccccn3)c2=O)c1F 10.1021/jm030472z
11294792 62958 0 None 380 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 62958 0 None 380 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
44309652 202602 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccccc4OC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL71400 202602 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 617 11 0 8 6.4 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccccc4OC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
11192019 13149 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human gonadotropin-releasing hormone receptorBinding affinity for human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
CHEMBL119149 13149 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity for human gonadotropin-releasing hormone receptorBinding affinity for human gonadotropin-releasing hormone receptor
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049218c
44576678 170481 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 11 1 7 5.8 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL445691 170481 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 617 11 1 7 5.8 COC(=O)CCCN[C@@H](Cn1c(=O)c(-c2ccccc2Cl)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
11192019 13149 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL119149 13149 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 509 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)Cc3ccccc3)c2=O)c1F 10.1021/jm049791w
44387888 60162 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3cccc(F)c3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL175491 60162 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3cccc(F)c3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
44388033 61433 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 497 7 1 9 2.1 COc1cccc(-n2c(=O)n(Cc3cccnc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL177182 61433 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 497 7 1 9 2.1 COc1cccc(-n2c(=O)n(Cc3cccnc3Cl)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21045823 113643 0 None 40 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL332923 113643 0 None 40 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 546 7 2 3 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNC(=O)C(F)(F)F)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44267865 160837 0 None -10 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
CHEMBL412634 160837 0 None -10 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 11 1 14 7.0 CC[C@H]1COC(=O)N1C(=O)O[C@H]1[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]2(C)[C@@H](CC)OC(=O)[C@@H]1C 10.1021/jm030418i
44400122 132840 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 2 6 3.5 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL370480 132840 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 467 6 2 6 3.5 N[C@@H](Cn1c(=O)c(-c2cccc(O)c2F)cn(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44432637 154433 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 492 8 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)c2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
CHEMBL401225 154433 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Displacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHRDisplacement of [125I]-Tyr5, DLeu6, NMeLeu7, Pro-N-Et-GnRH from cloned rat GnRHR
ChEMBL 492 8 2 3 5.8 Cc1cc(C)cc(-c2[nH]c3c(c2[C@H](C)CNCCc2ccncc2)CN(C(=O)c2ccccc2)CC3)c1 10.1016/j.bmcl.2007.05.009
44352641 117660 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 605 12 0 10 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL340856 117660 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 605 12 0 10 5.0 CCOC(=O)c1cn(Cc2ccccc2OC)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL263690 208841 0 None - 1 Rat 7.2 pKi = 7.2 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H]1CC(=O)NC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC(=O)[C@H](Cc2cccnc2)NC1=O 10.1021/jm990116+
11444384 63089 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1016/j.bmcl.2004.02.004
CHEMBL179663 63089 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1016/j.bmcl.2004.02.004
CHEMBL311380 63089 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccc(F)c1 10.1016/j.bmcl.2004.02.004
44309404 102276 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 648 10 0 8 6.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2F)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL305034 102276 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 648 10 0 8 6.9 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN(C)CCc2ccccc2F)cc1 10.1016/s0960-894x(02)00371-2
21045817 114052 0 None 22 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333730 114052 0 None 22 2 Human 7.2 pKi = 7.2 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 528 8 2 5 7.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CNc4ncccn4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44448860 94621 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
CHEMBL255242 94621 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NC3CCCC3)c2=O)c1F 10.1016/j.bmcl.2008.04.029
11295556 98793 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.3 CCOc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
CHEMBL281776 98793 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 534 11 0 7 4.3 CCOc1ccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)CCc3ccccn3)c2=O)cc1 10.1021/jm030472z
44576642 187211 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 513 7 2 6 4.1 N[C@@H](Cn1c(=O)c(-c2ccc(CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL495882 187211 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 513 7 2 6 4.1 N[C@@H](Cn1c(=O)c(-c2ccc(CO)cc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44434437 150441 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
CHEMBL395826 150441 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 42 6 27 8.5 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCc2cn(CCOCCOCCOCCn3cc(CNC(=O)CN(Cc4ccccc4)Cc4c(-c5ccc(NC(=O)NCC)cc5)nc5n(Cc6c(F)cccc6F)cc(C(=O)OCC)c(=O)n45)nn3)nn2)Cc2ccccc2)cc1 10.1016/j.bmc.2007.04.065
44267863 98066 0 None -2 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL276217 98066 0 None -2 2 Rat 6.2 pKi = 6.2 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 950 12 1 14 7.7 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@H]2CC(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11353175 99020 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 537 9 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283170 99020 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 537 9 1 6 5.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1F 10.1021/jm030472z
44394616 66026 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 617 9 2 9 5.7 CCOC(=O)Nc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
CHEMBL185143 66026 0 None - 1 Human 8.2 pKi = 8.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 617 9 2 9 5.7 CCOC(=O)Nc1ccc(-c2nc(-c3c(C)n(Cc4c(F)cccc4F)c(=O)n(C[C@H](N)c4ccccc4)c3=O)cs2)cc1 10.1016/j.bmcl.2004.07.022
21047618 114032 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333574 114032 0 None 1 2 Rat 8.2 pKi = 8.2 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 635 11 3 7 7.8 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ncc(C)c(NCC5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44288082 162618 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 981 10 1 14 8.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL418067 162618 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 981 10 1 14 8.2 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OC[C@@H]2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)c(Cl)c3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44449153 154537 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
CHEMBL401807 154537 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 581 9 1 6 6.2 CC[C@H](Cn1c(=O)c(-c2cccc(OC)c2Cl)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)NC1CCCC1 10.1016/j.bmcl.2008.04.029
10439419 101713 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL302769 101713 0 None - 1 Human 8.1 pKi = 8.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00370-0
10439419 101713 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm701249f
CHEMBL302769 101713 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1021/jm701249f
11477615 121630 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 503 9 0 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CC(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL359682 121630 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 503 9 0 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](CC(C)C)N(C)C)c2=O)c1F 10.1021/jm049218c
10439419 101713 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL302769 101713 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 666 15 1 9 6.5 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OC(CC)CC)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
44587394 171906 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
CHEMBL448253 171906 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 599 11 2 7 5.1 Cc1c(-c2cccc(OCCCC(=O)O)c2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1C(F)(F)F 10.1016/j.bmcl.2008.07.059
21047583 15128 0 None 10 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121367 15128 0 None 10 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44288073 168860 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 965 12 2 14 7.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL442482 168860 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 965 12 2 14 7.1 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C3CCCC3)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
25156669 188541 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 13 2 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL510538 188541 0 None - 1 Human 8.1 pKi = 8.1 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 645 13 2 7 5.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCCCCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
44400121 126896 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
CHEMBL365985 126896 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.04.036
44400121 126896 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL365985 126896 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 483 6 1 5 4.6 N[C@@H](Cn1c(=O)c(-c2ccccc2)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11050145 192764 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 581 10 0 7 6.4 CCN(CCc1ccccn1)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
CHEMBL52506 192764 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 581 10 0 7 6.4 CCN(CCc1ccccn1)Cc1c(C(C)(C)C)nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n12 10.1021/jm0205402
11387100 10141 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL116074 10141 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049218c
11387100 10141 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL116074 10141 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 537 9 0 6 4.6 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](Cc3ccccc3)N(C)C)c2=O)c1F 10.1021/jm049791w
44267866 96665 0 None 4 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL267568 96665 0 None 4 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 907 10 1 14 6.6 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CC(C)OC2=O)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11179922 86892 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
CHEMBL23321 86892 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1021/jm030472z
44394896 65973 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 545 8 2 8 5.2 Cc1c(-c2csc(Nc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL184855 65973 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 545 8 2 8 5.2 Cc1c(-c2csc(Nc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
11179922 86892 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23321 86892 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 519 9 1 6 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3C)c2=O)c1 10.1016/s0960-894x(03)00619-x
44436019 167088 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 4.9 CN(C)[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
CHEMBL430171 167088 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 564 8 0 6 4.9 CN(C)[C@@H](Cn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(Cl)cc1)C2)c1ccccc1 10.1016/j.bmc.2007.05.029
44387945 122201 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL360447 122201 0 None - 1 Human 7.2 pKi = 7.2 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 494 8 1 8 2.6 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
11157017 121874 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1016/j.bmcl.2004.02.004
CHEMBL360056 121874 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1016/j.bmcl.2004.02.004
CHEMBL72199 121874 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1016/j.bmcl.2004.02.004
20728209 122807 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 443 5 1 6 3.5 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL361619 122807 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 443 5 1 6 3.5 NC(Cn1c(=O)c(-c2ccccc2F)c2n(c1=O)C(c1ccccc1)CO2)c1ccccc1 10.1016/j.bmcl.2005.01.009
44451294 95670 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1647 38 8 18 11.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260318 95670 0 None - 1 Human 6.2 pKi = 6.2 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1647 38 8 18 11.4 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21045831 10395 0 None 7 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL116611 10395 0 None 7 2 Human 6.2 pKi = 6.2 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 422 5 2 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCNCC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL2370251 208071 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
CHEMBL329695 209573 0 None - 1 Rat 6.2 pKi = 6.2 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@@H]1NC(=O)[C@@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H]([C@@H](C)CC)NC1=O 10.1021/jm990432o
44340860 9524 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112625 9524 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 9 0 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CN(C)CC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11363829 10080 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL115965 10080 0 None - 1 Human 7.2 pKi = 7.2 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 489 7 1 6 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)CC(C)(C)C)c2=O)c1F 10.1021/jm049791w
25156399 188461 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 603 10 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
CHEMBL509440 188461 0 None - 1 Human 7.2 pKi = 7.2 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from human GnRH receptor expressed in HEK293 cells by liquid scintillation counting
ChEMBL 603 10 2 7 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](NCC(=O)O)c3ccccc3)c2=O)c1F 10.1021/jm8006454
9915597 183608 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 552 8 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccc4)n3c2=O)c1 10.1021/jm0205402
CHEMBL48316 183608 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 552 8 0 6 6.6 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)C)c(CN(C)Cc4ccccc4)n3c2=O)c1 10.1021/jm0205402
44340840 112825 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1ccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)cc1 10.1016/s0960-894x(03)00619-x
CHEMBL331592 112825 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 535 10 1 7 4.7 COc1ccc(CNC[C@@H](C)n2c(=O)c(-c3cccc(OC)c3)c(C)n(Cc3c(F)cccc3F)c2=O)cc1 10.1016/s0960-894x(03)00619-x
CHEMBL405420 210812 0 None - 1 Rat 6.1 pKi = 6.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC[C@H](NC(C)=O)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]1CCC(=O)NCCCC[C@@H](C(=O)N2CCC[C@@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44451486 157632 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)cc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL408760 157632 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1691 34 8 20 10.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H](NC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)C(C)C)cc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44388026 129296 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 521 7 1 9 2.6 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL367548 129296 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 521 7 1 9 2.6 COc1cccc(-n2c(=O)n(Cc3c(Cl)cccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047858 9993 0 None -17 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL115425 9993 0 None -17 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CN)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
9891852 10953 0 None -18 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117736 10953 0 None -18 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 492 7 3 3 5.3 Cc1cc2c(cc1Cc1ccc(C(=O)NC[C@H]3CC[C@@H](CN=C(N)N)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
10439527 168913 0 None -288 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL443027 168913 0 None -288 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 677 15 0 9 7.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11214294 121681 0 None 912 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL359754 121681 0 None 912 2 Human 7.1 pKi = 7.1 Binding
Binding affinity for Monkey gonadotropin-releasing hormone receptorBinding affinity for Monkey gonadotropin-releasing hormone receptor
ChEMBL 505 6 1 7 3.8 Cc1c(-c2ccc3c(c2)OCCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
21045828 14395 0 None -2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL120420 14395 0 None -2 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 627 11 3 7 7.6 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNc4nccc(NCC5CCCO5)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44451408 95749 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL260750 95749 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)cc2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11214295 86562 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
CHEMBL23237 86562 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1021/jm030472z
11214295 86562 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL23237 86562 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 505 9 1 6 4.7 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3)c2=O)c1 10.1016/s0960-894x(03)00619-x
11341990 62171 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.bmcl.2004.02.004
CHEMBL178127 62171 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.bmcl.2004.02.004
CHEMBL76277 62171 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 447 6 1 5 4.0 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccc(F)cc1 10.1016/j.bmcl.2004.02.004
44387898 60719 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 508 8 1 8 2.9 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL176284 60719 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 508 8 1 8 2.9 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3C)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
10051739 85008 0 None -501 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL22653 85008 0 None -501 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 501 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCCC3)c2=O)c1F 10.1021/jm030472z
44346662 113927 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 633 12 0 9 5.9 CCN(CC)CCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL333213 113927 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 633 12 0 9 5.9 CCN(CC)CCN(C)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44352652 116981 0 None -245 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL339968 116981 0 None -245 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 689 14 0 9 7.6 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC4CCCC4)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
11282957 121819 0 None -1096 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
CHEMBL359894 121819 0 None -1096 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 477 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1 10.1021/jm049218c
9983568 98525 0 None -263 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL279885 98525 0 None -263 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 503 10 1 6 4.6 CCC(CC)N[C@@H](C)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44576655 187638 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 9 2 8 3.6 NCC(=O)OCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
CHEMBL499307 187638 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity to human GnRHRBinding affinity to human GnRHR
ChEMBL 570 9 2 8 3.6 NCC(=O)OCc1ccc(-c2cn(Cc3c(F)cccc3C(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)cc1 10.1016/j.bmcl.2008.04.036
11238091 62177 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1016/j.bmcl.2004.02.004
CHEMBL178142 62177 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1016/j.bmcl.2004.02.004
CHEMBL311407 62177 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells using des-Gly10-[125I]Tyr,5 DLeu,6 NMeLeu,7 Pro9-NEt GnRH as radioligand.
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1ccccn1 10.1016/j.bmcl.2004.02.004
44451379 168414 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL439076 168414 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 884 17 4 10 6.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N[C@H](C(=O)NCC#Cc2ccccc2)C(C)C)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352665 117771 0 None -43 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL340934 117771 0 None -43 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 635 13 0 9 6.3 CCC(CC)OC(=O)c1cn(Cc2ccccc2F)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
10875519 188724 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 575 8 0 9 3.9 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCN(C)CC1 10.1021/jm0205402
CHEMBL51232 188724 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 575 8 0 9 3.9 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCN(C)CC1 10.1021/jm0205402
11294792 62958 0 None -380 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
CHEMBL179269 62958 0 None -380 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 8 1 6 4.3 CN[C@@H](Cn1c(=O)c(-c2cccc(OC)c2)c(C)n(Cc2c(F)cccc2F)c1=O)c1ccccc1 10.1021/jm049218c
11455176 98602 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL280430 98602 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11455176 98602 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL280430 98602 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
44341074 9850 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL114619 9850 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 469 9 1 6 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCC3CC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
21045807 16138 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 8 2 5 7.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(C(F)(F)F)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL122653 16138 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 590 8 2 5 7.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(C(F)(F)F)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
11226171 87022 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL23337 87022 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11226171 87022 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
CHEMBL23337 87022 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 520 10 1 7 3.9 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCCc3ccccn3)c2=O)c1 10.1021/jm030472z
44309617 202259 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 605 10 0 7 6.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL69361 202259 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 605 10 0 7 6.5 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4cccc(F)c4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(02)00371-2
21047937 110809 0 None 1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL326606 110809 0 None 1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 472 7 1 3 6.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3ccc(CN(C)C)cc3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44288079 99750 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 896 11 3 14 5.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](NC)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
CHEMBL288396 99750 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity against human luteinizing releasing hormone receptor cloned in CHO cellsBinding affinity against human luteinizing releasing hormone receptor cloned in CHO cells
ChEMBL 896 11 3 14 5.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](NC)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1016/j.bmcl.2003.12.059
44267870 97669 0 None -8 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273536 97669 0 None -8 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11421518 164744 0 None -1047 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
CHEMBL423291 164744 0 None -1047 2 Rat 5.1 pKi = 5.1 Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptorIn vivo inhibition of rat Gonadotropin-releasing hormone receptor
ChEMBL 553 10 1 7 4.8 COc1ccccc1CNC[C@@H](C)n1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm030472z
44267904 97964 0 None -6 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL275521 97964 0 None -6 2 Human 6.1 pKi = 6.1 Binding
In vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to human luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 893 10 1 13 6.5 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2CCOC2C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
11103767 101324 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 569 10 1 8 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CO)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
CHEMBL300079 101324 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 569 10 1 8 5.0 COc1cccc(-c2c(C)n(Cc3ccccc3F)c3nc(C(C)(C)CO)c(CN(C)Cc4ccccn4)n3c2=O)c1 10.1021/jm0205402
44400188 69037 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 501 6 1 5 4.7 N[C@@H](Cn1c(=O)c(-c2ccccc2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL193031 69037 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 501 6 1 5 4.7 N[C@@H](Cn1c(=O)c(-c2ccccc2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
44347047 16422 0 None -5 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL124056 16422 0 None -5 2 Human 8.1 pKi = 8.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(NC[C@@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
9984259 110012 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
CHEMBL324912 110012 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm701249f
9984259 110012 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
CHEMBL324912 110012 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049218c
9984259 110012 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
CHEMBL324912 110012 0 None 281 2 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.3 CN[C@@H](Cc1ccccc1)Cn1c(=O)c(-c2cccc(OC)c2F)c(C)n(Cc2c(F)cccc2F)c1=O 10.1021/jm049791w
44400353 68332 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 599 8 1 6 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCC(F)(F)F)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
CHEMBL192096 68332 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 599 8 1 6 5.7 N[C@@H](Cn1c(=O)c(-c2cccc(OCC(F)(F)F)c2F)cn(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2005.03.057
11307227 122537 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 6 5.8 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL360935 122537 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 539 8 1 6 5.8 Cc1c(-c2ccc(Oc3ccccc3)cc2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL2371513 208319 0 None - 1 Rat 8.1 pKi = 8.1 Binding
Competitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptorCompetitive radioligand binding assay, in human HEK293 cells stably transfected with the rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@H](Cc1cccnc1)C(=O)N[C@H](CC(=O)O)C(=O)N[C@H]1CCC(=O)NCCC[C@H](C(=O)N2CCC[C@H]2C(=O)N[C@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CCCN=C(N)N)NC1=O 10.1021/jm990115h
44267870 97669 0 None 8 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
CHEMBL273536 97669 0 None 8 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cellsIn vitro binding affinity to rat luteinizing hormone-releasing hormone (LHRH) receptor cloned in CHO cells
ChEMBL 921 10 1 14 7.0 CC[C@H]1OC(=O)[C@H](C)[C@@H](OC(=O)N2C(=O)OCC2(C)C)[C@H](C)[C@@H](OC2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@@](C)(OC)C[C@@H](C)C(=O)[C@H](C)[C@H]2N(CCc3ccc(Cl)cc3)C(=O)O[C@]12C 10.1021/jm030418i
44309319 202019 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 609 12 1 8 5.9 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
CHEMBL67638 202019 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 609 12 1 8 5.9 CCCC(=O)Nc1ccc(-c2nc3n(Cc4ccccc4F)cc(C(=O)OCC)c(=O)n3c2CN(C)Cc2ccccc2)cc1 10.1016/s0960-894x(02)00370-0
44435992 96060 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 597 10 0 8 4.8 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
CHEMBL262581 96060 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 597 10 0 8 4.8 Cc1c(CN2CCc3c(c(=O)n(CCN(C)CCc4ccccn4)c(=O)n3Cc3ccccc3F)C2)sc2ccccc12 10.1016/j.bmc.2007.05.029
21047583 15128 0 None -10 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL121367 15128 0 None -10 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 607 9 2 7 6.7 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4nccc(N5CCOCC5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44352679 115002 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL335196 115002 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 653 13 0 9 6.2 CCOC(=O)c1cn(Cc2c(F)cccc2F)c2c(C#N)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44387920 63553 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3F)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL180421 63553 0 None - 1 Human 6.1 pKi = 6.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccccc3F)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL2370261 208077 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](N)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(=O)O)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
CHEMBL329946 209577 0 None - 1 Rat 5.1 pKi = 5.1 Binding
Inhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranesInhibition constant for the displacement of specific binding of [125I][D-Lys6]-GnRH (Kd=177 pM) bound to rat pituitary membranes
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](N)Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)O)[C@@H](C)CC 10.1021/jm990432o
44435981 146416 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 623 11 0 9 2.9 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL392603 146416 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 623 11 0 9 2.9 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccc(S(C)(=O)=O)cc1)C2 10.1016/j.bmc.2007.05.029
44340641 110088 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 529 13 1 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL325391 110088 0 None - 1 Human 7.1 pKi = 7.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 529 13 1 7 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CC(C)NCCCOCC(C)C)c2=O)c1 10.1016/s0960-894x(03)00620-6
11260704 98222 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2ccccc2F)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
CHEMBL277439 98222 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity evaluated by the ability to inhibit des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]- Gonadotropin-releasing hormone binding to cloned human Gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 508 9 0 6 4.0 Cc1c(-c2ccccc2F)c(=O)n(CCN(C)CCc2ccccn2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm030472z
44451446 168151 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL436862 168151 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1663 36 8 20 10.1 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
11249548 98633 0 None 97 2 Human 6.1 pKi = 6.1 Binding
In vivo inhibition of monkey Gonadotropin releasing hormone receptorIn vivo inhibition of monkey Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
CHEMBL280664 98633 0 None 97 2 Human 6.1 pKi = 6.1 Binding
In vivo inhibition of monkey Gonadotropin releasing hormone receptorIn vivo inhibition of monkey Gonadotropin releasing hormone receptor
ChEMBL 530 9 1 8 4.1 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](C)NCc3nccs3)c2=O)c1F 10.1021/jm030472z
44387922 60222 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccc(F)cc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
CHEMBL175869 60222 0 None - 1 Human 7.1 pKi = 7.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 512 8 1 8 2.7 COc1cccc(-n2c(=O)n(CCC(N)c3ccc(F)cc3)c(=O)n(Cc3c(F)cccc3F)c2=O)c1 10.1016/j.bmcl.2005.05.038
9823968 109992 0 None -1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
CHEMBL324771 109992 0 None -1 2 Human 7.1 pKi = 7.1 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 429 5 1 2 6.8 Cc1ccc(CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)cc1 10.1016/s0960-894x(02)00755-2
21046570 112588 0 None -34 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
CHEMBL331277 112588 0 None -34 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 479 6 1 4 6.2 COC(=O)[C@H]1CC[C@H](CNC(=O)c2ccc(Cc3cc4c(cc3C)C(C)(C)CCC4(C)C)o2)CC1 10.1016/s0960-894x(02)00755-2
44340643 110856 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 8 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(CCc4ccccn4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL326885 110856 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 532 8 0 7 4.2 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C3CCN(CCc4ccccn4)C3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44451343 96019 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1591 34 8 18 9.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL262335 96019 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1591 34 8 18 9.9 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCCCC(=O)NCC#Cc2ccccc2C#CCNC(=O)CCCNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44340824 9381 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3cccc(F)c3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL111933 9381 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3cccc(F)c3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44435984 88352 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
CHEMBL236332 88352 0 None - 1 Human 7.1 pKi = 7.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 559 10 0 7 3.8 Cc1ccccc1CN1CCc2c(c(=O)n(CCN(C)CCc3ccccn3)c(=O)n2Cc2c(F)cccc2F)C1 10.1016/j.bmc.2007.05.029
44435983 88351 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1cccc(Cl)c1)C2 10.1016/j.bmc.2007.05.029
CHEMBL236331 88351 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 579 10 0 7 4.1 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1cccc(Cl)c1)C2 10.1016/j.bmc.2007.05.029
44451258 166872 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1729 32 8 20 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL429690 166872 0 None - 1 Human 6.1 pKi = 6.1 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1729 32 8 20 8.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)ccc(=O)n3c2CN(CC(=O)NCC(=O)N2CCC[C@H]2C(=O)NCC#Cc2ccccc2C#CCNC(=O)[C@@H]2CCCN2C(=O)CNC(=O)CN(Cc2ccccc2)Cc2c(-c3ccc(NC(=O)NCC)cc3)nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n23)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44352942 22411 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 609 11 0 9 5.6 CCOC(=O)c1cn(Cc2ccccc2Cl)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
CHEMBL132661 22411 0 None - 1 Human 5.1 pKi = 5.1 Binding
Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.Binding affinity against human GnRH receptor expressed in HEK293 cells using des-Gly10[125I]Tyr5, D-Leu, NMeLeu, Pro-NEt GnRH as radioligand.
ChEMBL 609 11 0 9 5.6 CCOC(=O)c1cn(Cc2ccccc2Cl)c2c(C#N)c(-c3ccc(OC)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(01)00779-x
44388018 60152 0 None 389 2 Human 7.1 pKi = 7.1 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL175443 60152 0 None 389 2 Human 7.1 pKi = 7.1 Binding
Inhibition constant against monkey GnRH receptorInhibition constant against monkey GnRH receptor
ChEMBL 487 7 1 9 1.9 COc1cccc(-n2c(=O)n(Cc3ccccc3C#N)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
21047784 110148 0 None -36 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL325747 110148 0 None -36 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 574 9 4 7 6.1 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCC(CNCc4cc(O)nc(O)n4)CC3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11191675 63052 0 None 186 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL179600 63052 0 None 186 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
CHEMBL3085404 63052 0 None 186 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 487 8 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NC3CCC3)c2=O)c1F 10.1021/jm030472z
11226531 99059 0 None 169 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
CHEMBL283381 99059 0 None 169 2 Human 7.1 pKi = 7.1 Binding
In vivo inhibition of monkey Gonadotropin-releasing hormone receptorIn vivo inhibition of monkey Gonadotropin-releasing hormone receptor
ChEMBL 543 9 1 7 5.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)NCc3sccc3C)c2=O)c1F 10.1021/jm030472z
44389647 64243 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 455 6 1 7 3.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1 10.1016/j.bmcl.2005.01.009
CHEMBL181582 64243 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 455 6 1 7 3.4 COc1cccc(-c2c3n(c(=O)n(CC(N)c4ccccc4)c2=O)C(c2ccccc2)CO3)c1 10.1016/j.bmcl.2005.01.009
44346665 112339 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 10 1 7 7.7 CC(C)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
CHEMBL330834 112339 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 636 10 1 7 7.7 CC(C)Nc1ccc(-c2sc3c(c2CN(C)Cc2ccccc2)c(=O)n(-c2ccccc2)c(=O)n3Cc2c(F)cccc2F)cc1 10.1016/s0960-894x(03)00746-7
11284357 60692 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1021/jm049218c
CHEMBL176270 60692 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1021/jm049218c
CHEMBL72913 60692 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 443 7 1 5 4.1 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CCc1ccccc1 10.1021/jm049218c
11329628 62695 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1021/jm049218c
CHEMBL178805 62695 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1021/jm049218c
CHEMBL73575 62695 0 None - 1 Human 6.1 pKi = 6.1 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 393 6 1 5 3.2 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1CC1CC1 10.1021/jm049218c
CHEMBL405837 210837 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@@H](CC(=O)NC[C@H](C(N)=O)NC(=O)[C@H]3CCCN3C(=O)[C@H](CCCN=C(N)N)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC2=O)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(Cl)cc2)NC1=O 10.1021/jm990116+
44390758 64615 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 468 6 1 7 2.3 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
CHEMBL182284 64615 0 None - 1 Human 7.1 pKi = 7.1 Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determinedInhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
ChEMBL 468 6 1 7 2.3 N[C@@H](Cn1c(=O)n(Cc2c(F)cccc2F)c(=O)n(-c2ccccc2F)c1=O)c1ccccc1 10.1016/j.bmcl.2004.11.026
44340652 9364 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL111820 9364 0 None - 1 Human 6.1 pKi = 6.1 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 534 10 0 7 4.3 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](C)N(C)CCc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
21047631 10858 0 None -5 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL117330 10858 0 None -5 2 Rat 6.1 pKi = 6.1 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 450 6 2 3 6.0 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(CN)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44352657 21351 0 None -269 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
CHEMBL131665 21351 0 None -269 2 Rat 5.1 pKi = 5.1 Binding
Binding affinity against gonadotropin-releasing hormone receptor of ratBinding affinity against gonadotropin-releasing hormone receptor of rat
ChEMBL 687 12 0 9 7.3 CN(CCc1ccccn1)Cc1c(-c2ccc(OC3CCCC3)cc2)c(C#N)c2n(Cc3ccccc3F)cc(C(=O)OC3CCCC3)c(=O)n12 10.1016/s0960-894x(01)00779-x
44387896 129152 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
CHEMBL367388 129152 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity at human GnRH receptorBinding affinity at human GnRH receptor
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1021/jm701249f
44394778 125366 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 8 1 7 5.1 Cc1c(-c2csc(Cc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
CHEMBL364842 125366 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligandBinding affinity towards cloned human Gonadotropin-releasing hormone receptor expressed in RBL cells was determined by using [125I]GnRH as radioligand
ChEMBL 544 8 1 7 5.1 Cc1c(-c2csc(Cc3ccccc3)n2)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1016/j.bmcl.2004.07.022
9852184 10589 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 628 13 0 8 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL117069 10589 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 628 13 0 8 6.4 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)CCc3ccccn3)n2c1=O 10.1016/s0960-894x(02)00745-x
44346396 112873 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 625 9 0 9 6.1 CN(Cc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
CHEMBL331762 112873 0 None - 1 Human 8.1 pKi = 8.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptorBinding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 625 9 0 9 6.1 CN(Cc1ccccn1)Cc1c(-c2ccc([N+](=O)[O-])cc2)sc2c1c(=O)n(-c1ccccc1)c(=O)n2Cc1c(F)cccc1F 10.1016/s0960-894x(03)00746-7
44387896 129152 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL367388 129152 0 None - 1 Human 8.1 pKi = 8.1 Binding
In vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cellsIn vitro ability to inhibit des-Gly[125I-Tyr, DLeu, NMeLeu,Pro-NEt]-GnRH radioligand binding to the cloned human GnRH receptor stably expressed in HEK293 cells
ChEMBL 498 7 1 8 2.3 COc1cccc(-n2c(=O)n(Cc3c(F)cccc3F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44347005 113966 0 None 6 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333461 113966 0 None 6 2 Rat 8.1 pKi = 8.1 Binding
In vitro binding affinity towards rat gonadotropin-releasing hormone receptorIn vitro binding affinity towards rat gonadotropin-releasing hormone receptor
ChEMBL 613 10 3 7 7.3 Cc1cc2c(cc1Cc1ccc(C(=O)NCC3CCCC(Nc4nccc(NCC5CCCO5)n4)C3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
44400247 121528 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 571 10 2 9 2.5 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)CCO)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
CHEMBL359558 121528 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligandBinding affinity towards human gonadotropin-releasing hormone receptor (GNRHR) using GnRH peptide as radioligand
ChEMBL 571 10 2 9 2.5 COc1cccc(-c2cn(Cc3c(F)cccc3S(=O)(=O)CCO)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.03.057
44353288 167794 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 662 13 2 7 6.4 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
CHEMBL434423 167794 0 None - 1 Human 8.0 pKi = 8.0 Binding
Binding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligandBinding affinity to human gonadotropin-releasing hormone (hGnRH) receptor expressed in HEK293 cells using des-Gly10[125I-Tyr,5DLeu,6NMeLeu,7Pro9-NEt]GnRH radioligand
ChEMBL 662 13 2 7 6.4 CCCC(=O)Nc1ccc(-c2cc3n(Cc4ccccc4F)cc(C(=O)NC4CCCC4)c(=O)n3c2CN(C)CCc2ccccn2)cc1 10.1016/s0960-894x(01)00780-6
44587403 188240 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 647 13 2 8 4.8 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL506338 188240 0 None - 1 Human 8.0 pKi = 8.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 647 13 2 8 4.8 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCOCC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
10394119 113949 0 None -1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL333345 113949 0 None -1 2 Human 8.0 pKi = 8.0 Binding
In vitro binding affinity towards human gonadotropin-releasing hormone receptorIn vitro binding affinity towards human gonadotropin-releasing hormone receptor
ChEMBL 621 11 3 7 7.5 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CNc4ccnc(NC[C@H]5CCCO5)n4)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00756-4
CHEMBL438712 212039 0 None - 1 Rat 8.0 pKi = 8 Binding
Affinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptorAffinity for rat gonadotrophin releasing hormone (GnRH) receptor using HEK293 cells transfected with rat Gonadotropin-releasing hormone receptor
ChEMBL None None None CC(=O)N[C@H](Cc1ccc2ccccc2c1)C(=O)N[C@@H](Cc1ccc(Cl)cc1)C(=O)N[C@@H]1CSSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](C)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc2ccc3ccccc3c2)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](C)NC1=O 10.1021/jm990116+
44340623 9389 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL111980 9389 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 523 9 1 6 4.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@H](C)CNCc3ccccc3F)c2=O)c1 10.1016/s0960-894x(03)00619-x
21047633 163922 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL421418 163922 0 None 1 2 Human 7.0 pKi = 7.0 Binding
In vitro binding affinity to human gonadotropin-releasing hormone receptorIn vitro binding affinity to human gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
44343881 10877 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 603 12 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
CHEMBL117346 10877 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human Gonadotropin-releasing hormone receptorBinding affinity towards human Gonadotropin-releasing hormone receptor
ChEMBL 603 12 0 8 6.5 CCOC(=O)c1cn(Cc2ccccc2F)c2c(F)c(-c3ccc(OCC(C)C)cc3)c(CN(C)Cc3ccco3)n2c1=O 10.1016/s0960-894x(02)00745-x
11082604 101289 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 608 8 0 8 5.7 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCc2ccccc2C1 10.1021/jm0205402
CHEMBL299850 101289 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding affinity against human gonadotropin-releasing hormone receptorBinding affinity against human gonadotropin-releasing hormone receptor
ChEMBL 608 8 0 8 5.7 COC(=O)C(C)(C)c1nc2n(Cc3ccccc3F)c(C)c(-c3cccc(OC)c3)c(=O)n2c1CN1CCc2ccccc2C1 10.1021/jm0205402
22716607 64448 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 493 5 1 6 4.9 NC(Cn1c(=O)c(-c2ccccc2Cl)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
CHEMBL181945 64448 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptorBinding affinity was determined against human gonadotropin-releasing hormone receptor
ChEMBL 493 5 1 6 4.9 NC(Cn1c(=O)c(-c2ccccc2Cl)c2n(c1=O)C(c1ccccc1F)CS2)c1ccccc1 10.1016/j.bmcl.2005.01.009
44451419 96500 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL266172 96500 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1687 30 6 20 10.3 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)N2CCC[C@H]2C(=O)NCC#Cc2cccc(C#CCNC(=O)[C@@H]3CCCN3C(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
44451430 155373 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
CHEMBL406084 155373 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]triptorelin from human GnRHR expressed in CHO cellsDisplacement of [125I]triptorelin from human GnRHR expressed in CHO cells
ChEMBL 1719 40 8 20 11.6 CCNC(=O)Nc1ccc(-c2nc3n(Cc4c(F)cccc4F)cc(C(=O)OCC)c(=O)n3c2CN(CC(=O)NCCCCCC(=O)NCC#Cc2cccc(C#CCNC(=O)CCCCCNC(=O)CN(Cc3ccccc3)Cc3c(-c4ccc(NC(=O)NCC)cc4)nc4n(Cc5c(F)cccc5F)cc(C(=O)OCC)c(=O)n34)c2)Cc2ccccc2)cc1 10.1016/j.bmc.2008.01.054
21047633 163922 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
CHEMBL421418 163922 0 None -1 2 Rat 7.0 pKi = 7.0 Binding
Binding affinity to rat gonadotropin-releasing hormone receptorBinding affinity to rat gonadotropin-releasing hormone receptor
ChEMBL 444 6 2 3 5.9 Cc1cc2c(cc1Cc1ccc(C(=O)NCc3cccc(CN)c3)o1)C(C)(C)CCC2(C)C 10.1016/s0960-894x(02)00755-2
11431754 13187 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
CHEMBL119185 13187 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 487 7 1 6 4.0 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C3CCCC3)c2=O)c1F 10.1021/jm049791w
44387961 165468 0 None -144 2 Rat 5.0 pKi = 5.0 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
CHEMBL425523 165468 0 None -144 2 Rat 5.0 pKi = 5.0 Binding
Inhibition constant against rat GnRH receptorInhibition constant against rat GnRH receptor
ChEMBL 546 8 1 9 3.0 COc1cccc(-n2c(=O)n(Cc3ccccc3OC(F)(F)F)c(=O)n(C[C@H](N)c3ccccc3)c2=O)c1F 10.1016/j.bmcl.2005.05.038
44436001 161133 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.6 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccc4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
CHEMBL413239 161133 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 598 8 0 6 5.6 Cc1ccc(CN2CCc3c(c(=O)n(CC4CCCCN4Cc4ccccc4)c(=O)n3Cc3c(F)cccc3F)C2)c(C)c1 10.1016/j.bmc.2007.05.029
44309671 202159 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 554 10 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
CHEMBL68664 202159 0 None - 1 Human 6.0 pKi = 6.0 Binding
Ability to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluatedAbility to inhibit [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt]GnRH agonist binding to the cloned human Gonadotropin-releasing hormone receptor was evaluated
ChEMBL 554 10 0 8 5.2 CCOC(=O)c1cn(Cc2ccccc2F)c2nc(-c3ccc(OC)cc3)c(CN(C)Cc3ccccc3)n2c1=O 10.1016/s0960-894x(02)00370-0
44340642 9578 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
CHEMBL112881 9578 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cellsBinding affinity towards human gonadotropin-releasing hormone receptor expressed in HEK293 cells
ChEMBL 483 8 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n([C@@H](C)CNC3CCCC3)c2=O)c1 10.1016/s0960-894x(03)00619-x
44309388 102073 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 609 7 0 9 5.2 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCCN(C)CC2)cc1 10.1016/s0960-894x(02)00371-2
CHEMBL304067 102073 0 None - 1 Human 5.0 pKi = 5.0 Binding
Binding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonistBinding evaluated in cloned human Gonadotropin-releasing hormone receptor by displacement of [125 I-Tyr, DLeu, NMeLeu, Pro-NEt]GnRH agonist
ChEMBL 609 7 0 9 5.2 COc1ccc(-c2nc3n(Cc4ccccc4F)c(C)c(-c4ccc5c(c4)OCO5)c(=O)n3c2CN2CCCN(C)CC2)cc1 10.1016/s0960-894x(02)00371-2
44340688 9518 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 0 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
CHEMBL112611 9518 0 None - 1 Human 7.0 pKi = 7.0 Binding
Ability to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cellsAbility to inhibit des-Gly10[125I]Tyr5,DLeu6,NMeLeu7, Pro9-NEt]-GnRH radioligand binding to the cloned human gonadotropin-releasing hormone receptor stably expressed in HEK293 cells
ChEMBL 506 9 0 7 3.8 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(CCN(C)Cc3ccccn3)c2=O)c1 10.1016/s0960-894x(03)00620-6
11489334 10393 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CCc3ccccc3)c2=O)c1F 10.1021/jm049791w
CHEMBL116576 10393 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 523 9 1 6 4.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)CCc3ccccc3)c2=O)c1F 10.1021/jm049791w
11294949 13927 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
CHEMBL119739 13927 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049218c
44435818 88676 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 399 4 1 6 2.0 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CNCC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL236545 88676 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 399 4 1 6 2.0 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CNCC3)c1 10.1016/j.bmc.2007.05.029
11294949 13927 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
CHEMBL119739 13927 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cellsBinding affinity towards human gonadotropin releasing hormone receptor using des-Gly10[125I]Tyr5,D-Leu6,NMeLeu7,Pro9-NEt]GnRH as radioligand expressed in HEK293 cells
ChEMBL 461 7 1 6 3.4 COc1cccc(-c2c(C)n(Cc3c(F)cccc3F)c(=O)n(C[C@@H](N)C(C)C)c2=O)c1F 10.1021/jm049791w
44587400 172602 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 13 2 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
CHEMBL452198 172602 0 None - 1 Human 7.0 pKi = 7.0 Binding
Displacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cellsDisplacement of [125I]tyr5,D-Leu6,NMeLeu7-GnRH from human cloned GnRH receptor expressed in RBL cells
ChEMBL 660 13 2 8 4.7 CN[C@@H](Cn1c(=O)c(-c2cccc(OCCN(C)CC(=O)O)c2F)c(C)n(Cc2c(F)cccc2C(F)(F)F)c1=O)c1ccccc1 10.1016/j.bmcl.2008.07.059
11157017 121874 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1021/jm049218c
CHEMBL360056 121874 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1021/jm049218c
CHEMBL72199 121874 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity for Human gonadotropin-releasing hormone receptorBinding affinity for Human gonadotropin-releasing hormone receptor
ChEMBL 430 6 1 6 3.3 Cc1c(-c2ccccc2F)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1cccnc1 10.1021/jm049218c
44435822 153657 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 519 7 0 7 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2OC)CC3)c1 10.1016/j.bmc.2007.05.029
CHEMBL398583 153657 0 None - 1 Human 6.0 pKi = 6.0 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 519 7 0 7 3.9 COc1cccc(-n2c(=O)c3c(n(Cc4c(F)cccc4F)c2=O)CN(Cc2ccccc2OC)CC3)c1 10.1016/j.bmc.2007.05.029
44435825 88076 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 545 10 0 7 3.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccccc1)C2 10.1016/j.bmc.2007.05.029
CHEMBL235084 88076 0 None - 1 Human 6.0 pKi = 6 Binding
Displacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cellsDisplacement of [125I]His5,D-Tyr6]GnRH from human cloned GnRH receptor transfected in COS7 cells
ChEMBL 545 10 0 7 3.5 CN(CCc1ccccn1)CCn1c(=O)c2c(n(Cc3c(F)cccc3F)c1=O)CCN(Cc1ccccc1)C2 10.1016/j.bmc.2007.05.029
11455317 62559 0 None -851 2 Rat 5.0 pKi = 5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
CHEMBL178457 62559 0 None -851 2 Rat 5.0 pKi = 5 Binding
Binding affinity for Rat gonadotropin-releasing hormone receptorBinding affinity for Rat gonadotropin-releasing hormone receptor
ChEMBL 491 6 1 7 3.7 Cc1c(-c2ccc3c(c2)OCO3)c(=O)n(C[C@H](N)c2ccccc2)c(=O)n1Cc1c(F)cccc1F 10.1021/jm049218c
11980076 206711 27 None - 1 Human 8.1 pIC50 = 8.1 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
CHEMBL1007 206711 27 None - 1 Human 8.1 pIC50 = 8.1 Binding
The Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptorThe Compound was tested for the concentration to inhibit 50% of [125 I ]leuprorelin binding to the cloned human Leutinizing releasing hormone receptor
Drug Central None None None CC(C)C[C@H](NC(=O)CNC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)NCC(N)=O None
1175 2266 38 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
1559 2266 38 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
657181 2266 38 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
CHEMBL1201199 2266 38 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
DB00007 2266 38 None - 1 Rat 8.0 pIC50 = 8.0 Binding
The compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitaryThe compound was tested for the concentration to inhibit 50% of [125 I]leuprorelin binding to Leutinizing releasing hormone receptor in the membrane fractions of the rat pituitary
Drug Central None None None None None
3823 49951 38 None -1 11 Rat 8.0 pKd = 8.0 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
76973198 49951 38 None -1 11 Rat 8.0 pKd = 8.0 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
CHEMBL157101 49951 38 None -1 11 Rat 8.0 pKd = 8.0 Binding
Dissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 MDissociation constant was determined in vitro using rat pituitary membranes and [125I]-leuprolide as radioligand, at concentration 3.16*10e-6 M
Drug Central 530 7 0 7 4.2 CC(=O)N1CCN(c2ccc(OCC3COC(Cn4ccnc4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 None
25077405 2675 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
3902 2675 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL1201309 2675 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
DB00666 2675 0 None - 1 Human 8.0 pKd = 8.0 Binding
NoneNone
Drug Central None None None None None
1162 1801 0 None 16 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
16132914 1801 0 None 16 2 Human 8.1 pKd = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3878 1803 0 None - 1 Human 8.2 pKd = 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17254668
188304 1601 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9341 1601 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272563 1601 0 None - 1 Human 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9342 323 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9855027 323 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272561 323 0 None - 1 Human 9.6 pKd = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9344 1903 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
25077495 1363 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9343 1363 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2365665 1363 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB11510 1363 0 None - 1 Human 9.7 pKd = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3860 733 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
3860 733 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
436 733 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
436 733 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
50225 733 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
50225 733 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
CHEMBL2110824 733 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2110824 733 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
DB06719 733 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB06719 733 0 None 57 2 Human 10.0 pKd = 10.0 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26774084
11167850 2701 22 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
1178 2701 22 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
1187 2701 22 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
CHEMBL179691 2701 22 None 6309 2 Human 9.7 pKd None 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 16930559
11250647 1516 40 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
5293 1516 40 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
8362 1516 40 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
CHEMBL1208155 1516 40 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
DB11979 1516 40 None -117 2 Rat 8.3 pKi = 8.3 Binding
Displacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation countingDisplacement of [125I-Tyr5,DLeu6,NMeLeu7,Pro9-NEt-]GnRH from rat GnRH receptor expressed in CHO cells by liquid scintillation counting
Drug Central 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F None
101755083 1332 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
16136245 1332 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
4379 1332 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
5585 1332 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL415606 1332 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
DB06699 1332 42 None - 1 Human 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
1190 869 41 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
25074887 869 41 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
583 869 41 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
CHEMBL1200490 869 41 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
DB00050 869 41 None - 1 Human 8.1 pKi = 8.1 Binding
GRAC: human GnRH1 selective antagonistGRAC: human GnRH1 selective antagonist
Drug Central None None None None None
1177 3806 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
25074470 3806 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
2968 3806 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
CHEMBL1201334 3806 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
DB06825 3806 0 None -10 2 Rat 8.1 pKi = 8.1 Binding
NoneNone
Drug Central None None None None None
1188 217 40 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
16131215 217 40 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
35 217 40 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
CHEMBL1252 217 40 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
DB00106 217 40 None - 1 Human 8.0 pKi = 8.0 Binding
NoneNone
Drug Central None None None None None
11225 1096 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.
Guide to Pharmacology 645 10 0 6 6.0 FCCOc1cccc(c1F)c1c(C)n(Cc2c(F)cccc2C(F)(F)F)c(=O)n(c1=O)C[C@H](N1CCCC1=O)c1ccccc1 32677155
154699464 1096 0 None - 1 Rat 8.3 pKi = 8.3 Binding
Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.Binding affinity to rat GnRH receptors as determined from competitive binding studies against [<sup>125</sup>I]buserelin.
Guide to Pharmacology 645 10 0 6 6.0 FCCOc1cccc(c1F)c1c(C)n(Cc2c(F)cccc2C(F)(F)F)c(=O)n(c1=O)C[C@H](N1CCCC1=O)c1ccccc1 32677155
1162 1801 0 None -16 2 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
16132914 1801 0 None -16 2 Rat 6.8 pKi = 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
1162 1801 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
1162 1801 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
16132914 1801 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
16132914 1801 0 None 16 2 Human 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1162 1801 0 None 16 2 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
16132914 1801 0 None 16 2 Human 8.1 pKi = 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
101755083 1332 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
16136245 1332 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
4379 1332 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
5585 1332 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
CHEMBL415606 1332 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
DB06699 1332 42 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21188095
1175 2266 38 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1559 2266 38 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
657181 2266 38 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1201199 2266 38 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00007 2266 38 None - 1 Human 8.8 pKi = 8.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
11250647 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
11250647 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
5293 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
5293 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
8362 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
8362 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
CHEMBL1208155 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
CHEMBL1208155 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
DB11979 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 19006286
DB11979 1516 40 None 117 2 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 631 12 2 7 5.5 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)NCCCC(=O)O)c(=O)n(c1C)Cc1c(F)cccc1C(F)(F)F 30194661
188304 1601 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9341 1601 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272563 1601 0 None - 1 Human 9.1 pKi = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9342 323 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9855027 323 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL3272561 323 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9344 1903 0 None - 1 Human 9.2 pKi = 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1188 217 40 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
16131215 217 40 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
35 217 40 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1252 217 40 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00106 217 40 None - 1 Human 9.3 pKi = 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1177 3806 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
25074470 3806 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
2968 3806 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
CHEMBL1201334 3806 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
DB06825 3806 0 None 10 2 Human 9.4 pKi = 9.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
101827019 2075 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
16130938 2075 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
3854 2075 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
73952264 2075 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
CHEMBL3989438 2075 0 None - 1 Human 9.5 pKi = 9.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 1850267
25077495 1363 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
9343 1363 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2365665 1363 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB11510 1363 0 None - 1 Human 9.6 pKi = 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1190 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1190 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
1190 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
25074887 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
25074887 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
25074887 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
583 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
583 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
583 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
CHEMBL1200490 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
CHEMBL1200490 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
CHEMBL1200490 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
DB00050 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
DB00050 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 7649152
DB00050 869 41 None - 1 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
3860 733 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
436 733 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
50225 733 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
CHEMBL2110824 733 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
DB06719 733 0 None 57 2 Human 9.7 pKi = 9.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26398856
1180 1276 0 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1185 3645 32 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
3038517 3645 32 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
CHEMBL22055 3645 32 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
DB06494 3645 32 None - 1 Human 10.0 pKi None 10 Binding
UnclassifiedUnclassified
Guide to Pharmacology 667 10 2 8 6.5 CONC(=O)Nc1ccc(cc1)c1sc2c(c1CN(Cc1ccccc1)C)c(=O)n(c(=O)n2Cc1c(F)cccc1F)c1ccccc1 12502365
1191 1262 0 None - 1 Human 7.9 pKi None 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1170 1900 0 None - 1 Human 8.1 pKi None 8.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 17095587
1179 947 31 None -4 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 12606616
9957278 947 31 None -4 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 12606616
CHEMBL494803 947 31 None -4 3 Human 8.2 pKi None 8.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 491 7 1 5 6.8 COc1cc(OC)c(c(c1)OC)NC(=O)c1ccc(o1)Cc1cc2c(cc1C)C(C)(C)CCC2(C)C 12606616
10279142 1596 0 None - 1 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1182 1596 0 None - 1 Human 8.3 pKi None 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 509 7 1 8 6.0 COc1nc(OC)c(c(n1)OC)NC(=O)c1ccc(o1)Oc1cc2c(cc1C)C(C)(C)C(CC2(C)C)C 18344315
1181 1277 0 None - 1 Human 8.6 pKi None 8.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
1177 3806 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
25074470 3806 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
2968 3806 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
CHEMBL1201334 3806 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
DB06825 3806 0 None -10 2 Rat 8.7 pKi None 8.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11726197
11167850 2701 22 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1178 2701 22 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1187 2701 22 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
CHEMBL179691 2701 22 None 6309 2 Human 9.2 pKi None 9.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
11167850 2701 22 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1178 2701 22 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1187 2701 22 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
CHEMBL179691 2701 22 None 6309 2 Human 9.3 pKi None 9.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 495 7 1 6 4.2 COc1cccc(c1F)c1c(=O)n(C[C@@H](c2ccccc2)N)c(=O)n(c1C)Cc1c(F)cccc1F 17095587
1189 423 0 None - 1 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077
16132443 423 0 None - 1 Human 9.6 pKi None 9.6 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 9300077