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Assay Detail

CHEMBL666549

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

Binding
Binding affinity for human recombinant corticotropin releasing factor receptor 1
79
Total Activities
77
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Corticotropin-releasing factor receptor 1 (CHEMBL1800)
Type SINGLE PROTEIN
Organism Homo sapiens

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 79 7.83 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL167407 1 8.70
CHEMBL168131 1 8.52
CHEMBL167463 1 8.40
CHEMBL168844 1 8.40
CHEMBL424555 1 8.40
CHEMBL166895 1 8.30
CHEMBL166345 1 8.30
CHEMBL353877 1 8.30
CHEMBL354367 1 8.30
CHEMBL167177 1 8.30
CHEMBL354178 1 8.30
CHEMBL167428 1 8.30
CHEMBL354395 1 8.30
CHEMBL166388 1 8.30
CHEMBL424538 1 8.22
CHEMBL166056 1 8.22
CHEMBL168497 1 8.22
CHEMBL168169 1 8.15
CHEMBL167095 1 8.15
CHEMBL422555 1 8.10
CHEMBL355544 1 8.10
CHEMBL442773 1 8.10
CHEMBL353973 1 8.05
CHEMBL10203 1 8.05
CHEMBL268993 1 8.05
CHEMBL167122 1 8.00
CHEMBL352378 1 8.00
CHEMBL167444 1 7.96
CHEMBL169094 1 7.96
CHEMBL46479 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL167407 Ki = 2.0 nM 8.70
CHEMBL168131 Ki = 3.0 nM 8.52
CHEMBL424555 Ki = 4.0 nM 8.40
CHEMBL168844 Ki = 4.0 nM 8.40
CHEMBL167463 Ki = 4.0 nM 8.40
CHEMBL166895 Ki = 5.0 nM 8.30
CHEMBL166345 Ki = 5.0 nM 8.30
CHEMBL354367 Ki = 5.0 nM 8.30
CHEMBL354178 Ki = 5.0 nM 8.30
CHEMBL167428 Ki = 5.0 nM 8.30
CHEMBL353877 Ki = 5.0 nM 8.30
CHEMBL354395 Ki = 5.0 nM 8.30
CHEMBL166388 Ki = 5.0 nM 8.30
CHEMBL167177 Ki = 5.0 nM 8.30
CHEMBL424538 Ki = 6.0 nM 8.22
CHEMBL166056 Ki = 6.0 nM 8.22
CHEMBL168497 Ki = 6.0 nM 8.22
CHEMBL168169 Ki = 7.0 nM 8.15
CHEMBL167095 Ki = 7.0 nM 8.15
CHEMBL422555 Ki = 8.0 nM 8.10
CHEMBL355544 Ki = 8.0 nM 8.10
CHEMBL442773 Ki = 8.0 nM 8.10
CHEMBL268993 Ki = 9.0 nM 8.05
CHEMBL10203 Ki = 9.0 nM 8.05
CHEMBL353973 Ki = 9.0 nM 8.05
CHEMBL167122 Ki = 10.0 nM 8.00
CHEMBL352378 Ki = 10.0 nM 8.00
CHEMBL169094 Ki = 11.0 nM 7.96
CHEMBL167444 Ki = 11.0 nM 7.96
CHEMBL46479 Ki = 12.0 nM 7.92
CHEMBL166835 Ki = 13.0 nM 7.89
CHEMBL165531 Ki = 14.0 nM 7.85
CHEMBL166235 Ki = 14.0 nM 7.85
CHEMBL354584 Ki = 15.0 nM 7.82
CHEMBL167853 Ki = 17.0 nM 7.77
CHEMBL354791 Ki = 17.0 nM 7.77
CHEMBL355055 Ki = 18.0 nM 7.75
CHEMBL350356 Ki = 19.0 nM 7.72
CHEMBL165991 Ki = 20.0 nM 7.70
CHEMBL168360 Ki = 20.0 nM 7.70
CHEMBL167737 Ki = 22.0 nM 7.66
CHEMBL166890 Ki = 22.0 nM 7.66
CHEMBL432496 Ki = 22.0 nM 7.66
CHEMBL165473 Ki = 23.0 nM 7.64
CHEMBL166238 Ki = 24.0 nM 7.62
CHEMBL167171 Ki = 24.0 nM 7.62
CHEMBL167195 Ki = 24.0 nM 7.62
CHEMBL166807 Ki = 25.0 nM 7.60
CHEMBL354859 Ki = 25.0 nM 7.60
CHEMBL165873 Ki = 26.0 nM 7.58