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Assay Detail

CHEMBL665734

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

Binding
Displacement of [125I]0-CRF from human Corticotropin releasing factor receptor 1 expressed in CHO cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Pyrazolo[1,5-a]pyrimidine CRF-1 receptor antagonists.
Wustrow DJ, Capiris T, Rubin R, Knobelsdorf JA, Akunne H, Davis MD, MacKenzie R, Pugsley TA, Zoski KT, Heffner TG, Wise LD.
Bioorg Med Chem Lett (1998) 8 : 2067 -2070
PubMed 9873487 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.40 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL65078 1 8.49
CHEMBL290762 1 8.30
CHEMBL305092 1 8.19
CHEMBL302645 1 7.96
CHEMBL292764 1 7.82
CHEMBL303789 1 7.40
CHEMBL303593 1 7.39
CHEMBL9946 CP-154526 1 7.25
CHEMBL292484 1 7.16
CHEMBL62533 1 7.11
CHEMBL65724 1 7.03
CHEMBL65574 1 6.67
CHEMBL65308 1 6.51
CHEMBL65195 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL65078 Ki = 3.2 nM 8.49
CHEMBL290762 Ki = 5.0 nM 8.30
CHEMBL305092 Ki = 6.4 nM 8.19
CHEMBL302645 Ki = 11.0 nM 7.96
CHEMBL292764 Ki = 15.0 nM 7.82
CHEMBL303789 Ki = 40.0 nM 7.40
CHEMBL303593 Ki = 41.0 nM 7.39
CHEMBL9946 CP-154526 Ki = 56.0 nM 7.25
CHEMBL292484 Ki = 69.0 nM 7.16
CHEMBL62533 Ki = 77.0 nM 7.11
CHEMBL65724 Ki = 93.0 nM 7.03
CHEMBL65574 Ki = 216.0 nM 6.67
CHEMBL65308 Ki = 310.0 nM 6.51
CHEMBL65195 Ki = 511.0 nM 6.29