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Assay Detail

CHEMBL687313

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

Binding
Binding affinity was determined towards human gonadotropin-releasing hormone receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Identification of 1-arylmethyl-3- (2-aminoethyl)-5-aryluracil as novel gonadotropin-releasing hormone receptor antagonists.
Zhu YF, Gross TD, Guo Z, Connors PJ, Gao Y, Tucci FC, Struthers RS, Reinhart GJ, Saunders J, Chen TK, Killam Bonneville AL, Chen C.
J Med Chem (2003) 46 : 2023 -2026
PubMed 12747774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 6.35 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22929 1 7.62
CHEMBL60153 1 7.52
CHEMBL23797 1 7.42
CHEMBL303140 1 6.89
CHEMBL417558 1 6.66
CHEMBL23900 1 6.64
CHEMBL22563 1 6.40
CHEMBL60618 1 6.32
CHEMBL303811 1 6.28
CHEMBL64252 1 5.96
CHEMBL293247 1 5.77
CHEMBL304002 1 5.66
CHEMBL64066 1 5.42
CHEMBL64273 1 5.32
CHEMBL64212 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22929 Ki = 24.0 nM 7.62
CHEMBL60153 Ki = 30.0 nM 7.52
CHEMBL23797 Ki = 38.0 nM 7.42
CHEMBL303140 Ki = 130.0 nM 6.89
CHEMBL417558 Ki = 220.0 nM 6.66
CHEMBL23900 Ki = 230.0 nM 6.64
CHEMBL22563 Ki = 400.0 nM 6.40
CHEMBL60618 Ki = 480.0 nM 6.32
CHEMBL303811 Ki = 530.0 nM 6.28
CHEMBL64252 Ki = 1100.0 nM 5.96
CHEMBL293247 Ki = 1700.0 nM 5.77
CHEMBL304002 Ki = 2200.0 nM 5.66
CHEMBL64066 Ki = 3800.0 nM 5.42
CHEMBL64273 Ki = 4800.0 nM 5.32
CHEMBL64212 Ki = 4800.0 nM 5.32