Assay Detail

CHEMBL862345

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Binding

Inhibition of PDGFRbeta at 10 uM

ChEMBL ↗

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Target

Platelet-derived growth factor receptor beta (CHEMBL1913) ↗

Open DB target context

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Platelet-derived growth factor receptor beta (CHEMBL1913) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Platelet-derived growth factor receptor beta

CHEMBL1913

Anchored from Assay target.

Protein identity Platelet-derived growth factor receptor beta

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
Confidence	9 — Direct single protein target
Curated By	Expert

Target

Platelet-derived growth factor receptor beta (CHEMBL1913) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of S-[5-amino-1-(4-fluorophenyl)-1H-pyrazol-4-yl]-[3-(2,3-dihydroxypropoxy)phenyl]methanone (RO3201195), an orally bioavailable and highly selective inhibitor of p38 MAP kinase.

Goldstein DM, Alfredson T, Bertrand J, Browner MF, Clifford K, Dalrymple SA, Dunn J, Freire-Moar J, Harris S, Labadie SS, La Fargue J, Lapierre JM, Larrabee S, Li F, Papp E, McWeeney D, Ramesha C, Roberts R, Rotstein D, San Pablo B, Sjogren EB, So OY, Talamas FX, Tao W, Trejo A, Villasenor A, Welch M, Welch T, Weller P, Whiteley PE, Young K, Zipfel S.
J Med Chem (2006) 49 : 1562 -1575
PubMed 16509574 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Kd	1	6.21	6.21

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL203567	RO-3201195	1.0	1	6.21

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL203567	RO-3201195	Kd	=	610.0	nM	6.21