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Assay Detail

CHEMBL923765

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

Binding
Binding affinity to human GnRHR
18
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

5-Aryluracils as potent GnRH antagonists-Characterization of atropisomers.
Zhao L, Guo Z, Chen Y, Hu T, Wu D, Zhu YF, Rowbottom M, Gross TD, Tucci FC, Struthers RS, Xie Q, Chen C.
Bioorg Med Chem Lett (2008) 18 : 3344 -3349
PubMed 18442905 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 8.31 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL256109 2 9.52
CHEMBL556355 1 9.44
CHEMBL179691 1 9.25
CHEMBL259906 1 9.21
CHEMBL403234 2 9.15
CHEMBL359894 1 8.49
CHEMBL404180 1 8.43
CHEMBL401632 1 8.38
CHEMBL22653 1 8.35
CHEMBL259907 1 8.35
CHEMBL407719 1 8.31
CHEMBL191817 1 8.28
CHEMBL401807 1 8.13
CHEMBL257599 1 7.70
CHEMBL403081 1 7.48
CHEMBL255242 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL256109 Ki = 0.3 nM 9.52
CHEMBL556355 Ki = 0.36 nM 9.44
CHEMBL179691 Ki = 0.56 nM 9.25
CHEMBL259906 Ki = 0.61 nM 9.21
CHEMBL403234 Ki = 0.7 nM 9.15
CHEMBL359894 Ki = 3.2 nM 8.49
CHEMBL404180 Ki = 3.7 nM 8.43
CHEMBL401632 Ki = 4.2 nM 8.38
CHEMBL22653 Ki = 4.5 nM 8.35
CHEMBL259907 Ki = 4.5 nM 8.35
CHEMBL407719 Ki = 4.9 nM 8.31
CHEMBL191817 Ki = 5.3 nM 8.28
CHEMBL401807 Ki = 7.4 nM 8.13
CHEMBL257599 Ki = 20.0 nM 7.70
CHEMBL403081 Ki = 33.0 nM 7.48
CHEMBL256109 Ki = 61.0 nM 7.21
CHEMBL255242 Ki = 68.0 nM 7.17
CHEMBL403234 Ki = 190.0 nM 6.72