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Assay Detail

CHEMBL839629

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

Binding
Inhibitory constant against cloned human Gonadotropin-releasing hormone receptor stably expressed in HEK293 cells was determined
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

A convenient one-pot synthesis of asymmetric 1,3,5-triazine-2,4,6-triones and its application towards a novel class of gonadotropin-releasing hormone receptor antagonists.
Guo Z, Wu D, Zhu YF, Tucci FC, Pontillo J, Saunders J, Xie Q, Struthers RS, Chen C.
Bioorg Med Chem Lett (2005) 15 : 693 -698
PubMed 15664839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.13 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL321376 1 8.96
CHEMBL2113012 1 8.64
CHEMBL23830 1 7.47
CHEMBL366701 1 7.43
CHEMBL182284 1 7.05
CHEMBL369723 1 6.92
CHEMBL182145 1 6.66
CHEMBL359741 1 6.42
CHEMBL179953 1 6.39
CHEMBL180352 1 5.38
CHEMBL369101 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL321376 Ki = 1.1 nM 8.96
CHEMBL2113012 Ki = 2.3 nM 8.64
CHEMBL23830 Ki = 34.0 nM 7.47
CHEMBL366701 Ki = 37.0 nM 7.43
CHEMBL182284 Ki = 89.0 nM 7.05
CHEMBL369723 Ki = 120.0 nM 6.92
CHEMBL182145 Ki = 220.0 nM 6.66
CHEMBL359741 Ki = 380.0 nM 6.42
CHEMBL179953 Ki = 410.0 nM 6.39
CHEMBL180352 Ki = 4200.0 nM 5.38
CHEMBL369101 Ki > 20000.0 nM -