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Assay Detail

CHEMBL830138

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

Binding
Binding affinity for corticotropin-releasing factor-1 expressed in leukocyte tyrosine kinase cells
24
Total Activities
24
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

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

Publication

Design and synthesis of tricyclic imidazo[4,5-b]pyridin-2-ones as corticotropin-releasing factor-1 antagonists.
Guo Z, Tellew JE, Gross RS, Dyck B, Grey J, Haddach M, Kiankarimi M, Lanier M, Li BF, Luo Z, McCarthy JR, Moorjani M, Saunders J, Sullivan R, Zhang X, Zamani-Kord S, Grigoriadis DE, Crowe PD, Chen TK, Williams JP.
J Med Chem (2005) 48 : 5104 -5107
PubMed 16078829 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 7.30 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL191090 1 8.96
CHEMBL190845 1 8.70
CHEMBL296641 ANTALARMIN 1 8.51
CHEMBL188907 1 8.35
CHEMBL190488 1 8.29
CHEMBL364680 1 8.10
CHEMBL365260 1 7.92
CHEMBL189780 1 7.77
CHEMBL190881 1 7.70
CHEMBL371348 1 7.64
CHEMBL191395 1 7.36
CHEMBL414664 1 7.24
CHEMBL364892 1 7.22
CHEMBL361242 1 6.89
CHEMBL364938 1 6.85
CHEMBL190757 1 6.82
CHEMBL364037 1 6.77
CHEMBL190037 1 6.72
CHEMBL190262 1 6.70
CHEMBL191188 1 6.34
CHEMBL190661 1 6.04
CHEMBL363152 1 6.00
CHEMBL365745 1 5.06
CHEMBL365973 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL191090 Ki = 1.1 nM 8.96
CHEMBL190845 Ki = 2.0 nM 8.70
CHEMBL296641 ANTALARMIN Ki = 3.1 nM 8.51
CHEMBL188907 Ki = 4.5 nM 8.35
CHEMBL190488 Ki = 5.1 nM 8.29
CHEMBL364680 Ki = 8.0 nM 8.10
CHEMBL365260 Ki = 12.0 nM 7.92
CHEMBL189780 Ki = 17.0 nM 7.77
CHEMBL190881 Ki = 20.0 nM 7.70
CHEMBL371348 Ki = 23.0 nM 7.64
CHEMBL191395 Ki = 44.0 nM 7.36
CHEMBL414664 Ki = 58.0 nM 7.24
CHEMBL364892 Ki = 60.0 nM 7.22
CHEMBL361242 Ki = 130.0 nM 6.89
CHEMBL364938 Ki = 140.0 nM 6.85
CHEMBL190757 Ki = 150.0 nM 6.82
CHEMBL364037 Ki = 170.0 nM 6.77
CHEMBL190037 Ki = 190.0 nM 6.72
CHEMBL190262 Ki = 200.0 nM 6.70
CHEMBL191188 Ki = 460.0 nM 6.34
CHEMBL190661 Ki = 920.0 nM 6.04
CHEMBL363152 Ki = 1000.0 nM 6.00
CHEMBL365745 Ki = 8800.0 nM 5.06
CHEMBL365973 Ki > 10000.0 nM -