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Assay Detail

CHEMBL828889

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

Binding
Binding affinity was determined against human gonadotropin-releasing hormone receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Efficient synthesis of bicyclic oxazolino- and thiazolino[3,2-c]pyrimidine-5,7-diones and its application to the synthesis of GnRH antagonists.
Pontillo J, Chen C.
Bioorg Med Chem Lett (2005) 15 : 1407 -1411
PubMed 15713397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.12 8.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL359894 1 8.64
CHEMBL360126 1 8.35
CHEMBL112466 1 8.26
CHEMBL362237 1 7.40
CHEMBL181945 1 7.03
CHEMBL179101 1 6.96
CHEMBL425529 1 6.90
CHEMBL362283 1 6.66
CHEMBL362025 1 6.64
CHEMBL178961 1 6.34
CHEMBL361619 1 6.16
CHEMBL181582 1 6.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL359894 Ki = 2.3 nM 8.64
CHEMBL360126 Ki = 4.5 nM 8.35
CHEMBL112466 Ki = 5.5 nM 8.26
CHEMBL362237 Ki = 40.0 nM 7.40
CHEMBL181945 Ki = 93.0 nM 7.03
CHEMBL179101 Ki = 110.0 nM 6.96
CHEMBL425529 Ki = 125.0 nM 6.90
CHEMBL362283 Ki = 220.0 nM 6.66
CHEMBL362025 Ki = 230.0 nM 6.64
CHEMBL178961 Ki = 460.0 nM 6.34
CHEMBL361619 Ki = 700.0 nM 6.16
CHEMBL181582 Ki = 870.0 nM 6.06