Assay Detail

CHEMBL994499

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Binding

Displacement of [125I]Tyr0-ovine CRF from CRF1 receptor in human IMR32 cells

ChEMBL ↗

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Target

Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗

Open DB target context

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Corticotropin-releasing factor receptor 1 (CHEMBL1800) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Corticotropin-releasing factor receptor 1

CHEMBL1800

Anchored from Assay target.

Protein identity Corticotropin-releasing factor receptor 1

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Cell Type	IMR-32
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Corticotropin-releasing factor receptor 1 (CHEMBL1800) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Synthesis and structure-activity relationships of 8-(pyrid-3-yl)pyrazolo[1,5-a]-1,3,5-triazines: potent, orally bioavailable corticotropin releasing factor receptor-1 (CRF1) antagonists.

Gilligan PJ, Clarke T, He L, Lelas S, Li YW, Heman K, Fitzgerald L, Miller K, Zhang G, Marshall A, Krause C, McElroy JF, Ward K, Zeller K, Wong H, Bai S, Saye J, Grossman S, Zaczek R, Arneric SP, Hartig P, Robertson D, Trainor G.
J Med Chem (2009) 52 : 3084 -3092
PubMed 19361209 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	2	8.53	8.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL526149	—	—	1	8.70
CHEMBL482950	PEXACERFONT	3.0	1	8.35

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL526149	—	IC50	=	2.0	nM	8.70
CHEMBL482950	PEXACERFONT	IC50	=	4.5	nM	8.35