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Assay Detail

CHEMBL680275

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

Binding
In vivo inhibition of rat Gonadotropin-releasing hormone receptor
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Gonadotropin-releasing hormone receptor (CHEMBL3066)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and structure-activity relationships of 1-arylmethyl-5-aryl-6-methyluracils as potent gonadotropin-releasing hormone receptor antagonists.
Guo Z, Zhu YF, Gross TD, Tucci FC, Gao Y, Moorjani M, Connors PJ, Rowbottom MW, Chen Y, Struthers RS, Xie Q, Saunders J, Reinhart G, Chen TK, Bonneville AL, Chen C.
J Med Chem (2004) 47 : 1259 -1271
PubMed 14971906 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.25 5.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23830 1 5.66
CHEMBL3085404 1 5.66
CHEMBL283381 1 5.50
CHEMBL22314 1 5.31
CHEMBL23969 1 5.19
CHEMBL22653 1 5.12
CHEMBL279885 1 5.12
CHEMBL423291 1 5.10
CHEMBL23729 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23830 Ki = 2200.0 nM 5.66
CHEMBL3085404 Ki = 2200.0 nM 5.66
CHEMBL283381 Ki = 3200.0 nM 5.50
CHEMBL22314 Ki = 4900.0 nM 5.31
CHEMBL23969 Ki = 6400.0 nM 5.19
CHEMBL22653 Ki = 7500.0 nM 5.12
CHEMBL279885 Ki = 7600.0 nM 5.12
CHEMBL423291 Ki = 7900.0 nM 5.10
CHEMBL23729 Ki = 25000.0 nM 4.60