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Assay Detail

CHEMBL935136

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

Binding
Displacement of [125I]oCRF from rat CRF1 after 2 hrs by Betaplate scintillation counter
17
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Corticotropin-releasing factor receptor 1 (CHEMBL4649)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists.
Chen YL, Obach RS, Braselton J, Corman ML, Forman J, Freeman J, Gallaschun RJ, Mansbach R, Schmidt AW, Sprouse JS, Tingley Iii FD, Winston E, Schulz DW.
J Med Chem (2008) 51 : 1385 -1392
PubMed 18288792 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.89 8.43
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL271197 2 8.43
CHEMBL270948 2 8.29
CHEMBL405198 2 8.25
CHEMBL273040 2 8.19
CHEMBL270738 2 8.17
CHEMBL269833 2 8.14
CHEMBL271370 2 7.51
CHEMBL271368 2 6.13
CHEMBL272617 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL271197 IC50 = 3.7 nM 8.43
CHEMBL271197 IC50 = 3.715 nM 8.43
CHEMBL270948 IC50 = 5.1 nM 8.29
CHEMBL270948 IC50 = 5.129 nM 8.29
CHEMBL405198 IC50 = 5.6 nM 8.25
CHEMBL405198 IC50 = 5.623 nM 8.25
CHEMBL273040 IC50 = 6.4 nM 8.19
CHEMBL273040 IC50 = 6.457 nM 8.19
CHEMBL270738 IC50 = 6.8 nM 8.17
CHEMBL270738 IC50 = 6.761 nM 8.17
CHEMBL269833 IC50 = 7.244 nM 8.14
CHEMBL269833 IC50 = 7.2 nM 8.14
CHEMBL271370 IC50 = 31.0 nM 7.51
CHEMBL271370 IC50 = 30.9 nM 7.51
CHEMBL271368 IC50 = 741.31 nM 6.13
CHEMBL271368 IC50 = 750.0 nM 6.12
CHEMBL272617 Activity - -