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Assay Detail

CHEMBL712412

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

Binding
The negative logarithm of the concentration of antagonist that inhibits 50% of the binding of 125 I-labeled leuprolide to the rat pituitary LHRH receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The effect of NMeTyr5 substitution in luteinizing hormone-releasing hormone antagonists.
Haviv F, Fitzpatrick TD, Nichols CJ, Swenson RE, Mort NA, Bush EN, Diaz G, Nguyen AT, Holst MR, Cybulski VA.
J Med Chem (1993) 36 : 928 -933
PubMed 8385226 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 10.41 10.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL409219 1 10.87
CHEMBL268397 1 10.63
CHEMBL263839 1 10.50
CHEMBL263840 1 10.48
CHEMBL268319 1 10.28
CHEMBL409990 1 10.21
CHEMBL438829 1 9.93

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL409219 Ki = 0.01349 nM 10.87
CHEMBL268397 Ki = 0.02344 nM 10.63
CHEMBL263839 Ki = 0.03162 nM 10.50
CHEMBL263840 Ki = 0.03311 nM 10.48
CHEMBL268319 Ki = 0.05248 nM 10.28
CHEMBL409990 Ki = 0.06166 nM 10.21
CHEMBL438829 Ki = 0.1175 nM 9.93