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Assay Detail

CHEMBL664193

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Binding
Binding affinity was measured on rat Corticotropin releasing factor receptor 1
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Corticotropin-releasing factor receptor 1 (CHEMBL4649)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Non-peptide corticotropin-releasing hormone antagonists: syntheses and structure-activity relationships of 2-anilinopyrimidines and -triazines.
Arvanitis AG, Gilligan PJ, Chorvat RJ, Cheeseman RS, Christos TE, Bakthavatchalam R, Beck JP, Cocuzza AJ, Hobbs FW, Wilde RG, Arnold C, Chidester D, Curry M, He L, Hollis A, Klaczkiewicz J, Krenitsky PJ, Rescinito JP, Scholfield E, Culp S, De Souza EB, Fitzgerald L, Grigoriadis D, Tam SW, Shen HL.
J Med Chem (1999) 42 : 805 -818
PubMed 10072679 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 6.33 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166162 1 7.42
CHEMBL167264 1 7.34
CHEMBL168568 1 7.02
CHEMBL166102 1 6.73
CHEMBL353075 1 5.96
CHEMBL168764 1 5.48
CHEMBL167217 1 5.44
CHEMBL444577 1 5.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166162 Ki = 38.0 nM 7.42
CHEMBL167264 Ki = 46.0 nM 7.34
CHEMBL168568 Ki = 96.0 nM 7.02
CHEMBL166102 Ki = 187.0 nM 6.73
CHEMBL353075 Ki = 1099.0 nM 5.96
CHEMBL168764 Ki = 3301.0 nM 5.48
CHEMBL167217 Ki = 3655.0 nM 5.44
CHEMBL444577 Ki = 5700.0 nM 5.24