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Assay Detail

CHEMBL666049

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

Binding
In vitro binding affinity to the CRF receptor in rat cortical homogenates
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Expert

Target

Corticotropin releasing factor receptor (CHEMBL2111360)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Imidazo[4,5-b]pyridines as corticotropin releasing factor receptor ligands.
Arvanitis AG, Rescinito JT, Arnold CR, Wilde RG, Cain GA, Sun JH, Yan JS, Teleha CA, Fitzgerald LW, McElroy J, Zaczek R, Hartig PR, Grossman S, Arneric SP, Gilligan PJ, Olson RE, Robertson DW.
Bioorg Med Chem Lett (2003) 13 : 125 -128
PubMed 12467631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 8.64 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL23959 1 9.70
CHEMBL430913 1 9.40
CHEMBL23342 1 9.30
CHEMBL22622 1 9.22
CHEMBL3085294 1 9.22
CHEMBL23439 1 9.15
CHEMBL431105 1 9.13
CHEMBL22433 1 9.10
CHEMBL23354 1 9.00
CHEMBL423475 1 9.00
CHEMBL23483 1 9.00
CHEMBL276971 1 8.96
CHEMBL23950 1 8.89
CHEMBL282289 1 8.85
CHEMBL23291 1 8.82
CHEMBL22213 1 8.74
CHEMBL280666 1 8.72
CHEMBL431886 1 8.64
CHEMBL23105 1 8.62
CHEMBL23178 1 8.62
CHEMBL23669 1 8.46
CHEMBL23630 1 8.33
CHEMBL279734 1 8.29
CHEMBL23898 1 8.17
CHEMBL23788 1 7.80
CHEMBL23112 1 7.68
CHEMBL444011 1 7.62
CHEMBL280665 1 7.08
CHEMBL23799 1 7.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL23959 Ki = 0.2 nM 9.70
CHEMBL430913 Ki = 0.4 nM 9.40
CHEMBL23342 Ki = 0.5 nM 9.30
CHEMBL22622 Ki = 0.6 nM 9.22
CHEMBL3085294 Ki = 0.6 nM 9.22
CHEMBL23439 Ki = 0.7 nM 9.15
CHEMBL431105 Ki = 0.74 nM 9.13
CHEMBL22433 Ki = 0.8 nM 9.10
CHEMBL23354 Ki = 1.0 nM 9.00
CHEMBL423475 Ki = 1.0 nM 9.00
CHEMBL23483 Ki = 1.0 nM 9.00
CHEMBL276971 Ki = 1.1 nM 8.96
CHEMBL23950 Ki = 1.3 nM 8.89
CHEMBL282289 Ki = 1.4 nM 8.85
CHEMBL23291 Ki = 1.5 nM 8.82
CHEMBL22213 Ki = 1.8 nM 8.74
CHEMBL280666 Ki = 1.9 nM 8.72
CHEMBL431886 Ki = 2.3 nM 8.64
CHEMBL23105 Ki = 2.4 nM 8.62
CHEMBL23178 Ki = 2.4 nM 8.62
CHEMBL23669 Ki = 3.5 nM 8.46
CHEMBL23630 Ki = 4.7 nM 8.33
CHEMBL279734 Ki = 5.1 nM 8.29
CHEMBL23898 Ki = 6.8 nM 8.17
CHEMBL23788 Ki = 15.8 nM 7.80
CHEMBL23112 Ki = 20.8 nM 7.68
CHEMBL444011 Ki = 24.0 nM 7.62
CHEMBL280665 Ki = 82.7 nM 7.08
CHEMBL23799 Ki = 95.6 nM 7.02