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Assay Detail

CHEMBL4430591

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of [125I]D-Trp6-LHRH from human GnRH receptor expressed in CHO-K1 cell membranes incubated for 1 hr by competitive binding assay
ChEMBL ↗
134
Total Activities
134
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Gonadotropin-releasing hormone receptor (CHEMBL1855) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of an Orally Bioavailable Gonadotropin-Releasing Hormone Receptor Antagonist.
Kim SM, Lee M, Lee SY, Park E, Lee SM, Kim EJ, Han MY, Yoo T, Ann J, Yoon S, Lee J, Lee J.
J Med Chem (2016) 59 : 9150 -9172
PubMed 27608177 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 134 8.46 9.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4585638 — — 1 9.85
CHEMBL4474379 — — 1 9.80
CHEMBL4566719 — — 1 9.77
CHEMBL4516712 — — 1 9.77
CHEMBL4582367 — — 1 9.64
CHEMBL4539811 — — 1 9.51
CHEMBL4447139 — — 1 9.49
CHEMBL4544693 — — 1 9.48
CHEMBL4474058 — — 1 9.42
CHEMBL4449450 — — 1 9.41
CHEMBL4526641 — — 1 9.41
CHEMBL4460880 — — 1 9.41
CHEMBL4443108 — — 1 9.39
CHEMBL4449332 — — 1 9.36
CHEMBL4436854 — — 1 9.35
CHEMBL4593521 — — 1 9.24
CHEMBL179691 — — 1 9.23
CHEMBL4446435 — — 1 9.22
CHEMBL4540232 — — 1 9.17
CHEMBL4563562 — — 1 9.04
CHEMBL4463476 — — 1 9.02
CHEMBL4446131 — — 1 9.00
CHEMBL4576169 — — 1 9.00
CHEMBL4456703 — — 1 8.97
CHEMBL4452347 — — 1 8.96
CHEMBL4522657 — — 1 8.96
CHEMBL4563686 — — 1 8.96
CHEMBL4464132 — — 1 8.94
CHEMBL4461692 — — 1 8.92
CHEMBL4550720 — — 1 8.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4585638 — IC50 = 0.14 nM 9.85
CHEMBL4474379 — IC50 = 0.16 nM 9.80
CHEMBL4566719 — IC50 = 0.17 nM 9.77
CHEMBL4516712 — IC50 = 0.17 nM 9.77
CHEMBL4582367 — IC50 = 0.23 nM 9.64
CHEMBL4539811 — IC50 = 0.31 nM 9.51
CHEMBL4447139 — IC50 = 0.32 nM 9.49
CHEMBL4544693 — IC50 = 0.33 nM 9.48
CHEMBL4474058 — IC50 = 0.38 nM 9.42
CHEMBL4460880 — IC50 = 0.39 nM 9.41
CHEMBL4526641 — IC50 = 0.39 nM 9.41
CHEMBL4449450 — IC50 = 0.39 nM 9.41
CHEMBL4443108 — IC50 = 0.41 nM 9.39
CHEMBL4449332 — IC50 = 0.44 nM 9.36
CHEMBL4436854 — IC50 = 0.45 nM 9.35
CHEMBL4593521 — IC50 = 0.58 nM 9.24
CHEMBL179691 — IC50 = 0.59 nM 9.23
CHEMBL4446435 — IC50 = 0.6 nM 9.22
CHEMBL4540232 — IC50 = 0.68 nM 9.17
CHEMBL4563562 — IC50 = 0.91 nM 9.04
CHEMBL4463476 — IC50 = 0.95 nM 9.02
CHEMBL4446131 — IC50 = 1.0 nM 9.00
CHEMBL4576169 — IC50 = 1.0 nM 9.00
CHEMBL4456703 — IC50 = 1.07 nM 8.97
CHEMBL4522657 — IC50 = 1.1 nM 8.96
CHEMBL4563686 — IC50 = 1.1 nM 8.96
CHEMBL4452347 — IC50 = 1.1 nM 8.96
CHEMBL4464132 — IC50 = 1.16 nM 8.94
CHEMBL4550720 — IC50 = 1.2 nM 8.92
CHEMBL4461692 — IC50 = 1.2 nM 8.92
CHEMBL4474116 — IC50 = 1.27 nM 8.90
CHEMBL4467407 — IC50 = 1.42 nM 8.85
CHEMBL4556717 — IC50 = 1.5 nM 8.82
CHEMBL4557575 — IC50 = 1.7 nM 8.77
CHEMBL4590493 — IC50 = 1.8 nM 8.74
CHEMBL4456937 — IC50 = 1.95 nM 8.71
CHEMBL4467261 — IC50 = 2.0 nM 8.70
CHEMBL4583933 — IC50 = 2.0 nM 8.70
CHEMBL4567165 — IC50 = 2.57 nM 8.59
CHEMBL4585969 — IC50 = 2.76 nM 8.56
CHEMBL4173938 — IC50 = 2.9 nM 8.54
CHEMBL4515452 — IC50 = 3.1 nM 8.51
CHEMBL4451280 — IC50 = 3.8 nM 8.42
CHEMBL4517137 — IC50 = 3.77 nM 8.42
CHEMBL4543788 — IC50 = 4.1 nM 8.39
CHEMBL4530350 — IC50 = 5.0 nM 8.30
CHEMBL4472942 — IC50 = 5.11 nM 8.29
CHEMBL4446997 — IC50 = 6.59 nM 8.18
CHEMBL4475210 — IC50 = 6.8 nM 8.17
CHEMBL4521118 — IC50 = 7.01 nM 8.15