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Assay Detail

CHEMBL3631938

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

Binding
Displacement of [125I]-Tyr0-sauvagine from CRF1 receptor (unknown origin)
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis, binding affinity, radiolabeling, and microPET evaluation of 4-(2-substituted-4-substituted)-8-(dialkylamino)-6-methyl-1-substituted-3,4-dihydropyrido[2,3-b]pyrazin-2(1H)-ones as ligands for brain corticotropin-releasing factor type-1 (CRF1) receptors.
Stehouwer JS, Bourke CH, Owens MJ, Voll RJ, Kilts CD, Goodman MM.
Bioorg Med Chem Lett (2015) 25 : 5111 -5114
PubMed 26456805 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.81 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL439883 SAUVAGINE 1 9.10
CHEMBL309138 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL439883 SAUVAGINE Ki = 0.8 nM 9.10
CHEMBL309138 Ki = 3.0 nM 8.52