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Assay Detail

CHEMBL1809497

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

Binding
Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in rat cortical membrane after 2 hrs by scintillation counting
2
Total Activities
2
Compounds Tested
1
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

Discovery of N-(1-ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl]amine 59 (NGD 98-2): an orally active corticotropin releasing factor-1 (CRF-1) receptor antagonist.
Hodgetts KJ, Ge P, Yoon T, De Lombaert S, Brodbeck R, Gulianello M, Kieltyka A, Horvath RF, Kehne JH, Krause JE, Maynard GD, Hoffman D, Lee Y, Fung L, Doller D.
J Med Chem (2011) 54 : 4187 -4206
PubMed 21618986 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.22 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL309138 1 8.42
CHEMBL1807053 1 8.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL309138 Ki = 3.8 nM 8.42
CHEMBL1807053 Ki = 9.8 nM 8.01