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Assay Detail

CHEMBL666044

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

Binding
Binding affinity at Corticotropin releasing factor receptor of rat cortical homogenates.
21
Total Activities
21
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

CRF ligands via Suzuki and Negishi couplings of 3-pyridyl boronic acids or halides with 2-benzyloxy-4-chloro-3-nitropyridine.
Arvanitis AG, Arnold CR, Fitzgerald LW, Frietze WE, Olson RE, Gilligan PJ, Robertson DW.
Bioorg Med Chem Lett (2003) 13 : 289 -291
PubMed 12482442 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 8.42 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97340 1 9.30
CHEMBL100157 1 9.22
CHEMBL328163 1 9.15
CHEMBL316624 1 9.15
CHEMBL431287 1 9.15
CHEMBL328851 1 9.10
CHEMBL99286 1 8.96
CHEMBL99151 1 8.80
CHEMBL420442 1 8.74
CHEMBL316470 1 8.72
CHEMBL98093 1 8.70
CHEMBL99239 1 8.68
CHEMBL318051 1 8.48
CHEMBL100330 1 8.18
CHEMBL99098 1 8.12
CHEMBL95265 1 8.04
CHEMBL99093 1 8.00
CHEMBL319945 1 7.77
CHEMBL431810 1 6.22
CHEMBL99146 1 5.98
CHEMBL99097 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97340 Ki = 0.5 nM 9.30
CHEMBL100157 Ki = 0.6 nM 9.22
CHEMBL328163 Ki = 0.7 nM 9.15
CHEMBL316624 Ki = 0.7 nM 9.15
CHEMBL431287 Ki = 0.7 nM 9.15
CHEMBL328851 Ki = 0.8 nM 9.10
CHEMBL99286 Ki = 1.1 nM 8.96
CHEMBL99151 Ki = 1.6 nM 8.80
CHEMBL420442 Ki = 1.8 nM 8.74
CHEMBL316470 Ki = 1.9 nM 8.72
CHEMBL98093 Ki = 2.0 nM 8.70
CHEMBL99239 Ki = 2.1 nM 8.68
CHEMBL318051 Ki = 3.3 nM 8.48
CHEMBL100330 Ki = 6.6 nM 8.18
CHEMBL99098 Ki = 7.5 nM 8.12
CHEMBL95265 Ki = 9.2 nM 8.04
CHEMBL99093 Ki = 10.1 nM 8.00
CHEMBL319945 Ki = 17.1 nM 7.77
CHEMBL431810 Ki = 602.0 nM 6.22
CHEMBL99146 Ki = 1045.0 nM 5.98
CHEMBL99097 Ki > 10000.0 nM -