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Assay Detail

CHEMBL2405972

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Binding
Inhibition of p38beta (unknown origin)
3
Total Activities
3
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

Mitogen-activated protein kinase 11 (CHEMBL3961)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The identification of novel p38α isoform selective kinase inhibitors having an unprecedented p38α binding mode.
Wrobleski ST, Lin S, Dhar TG, Dyckman AJ, Li T, Pitt S, Zhang R, Fan Y, Doweyko AM, Tokarski JS, Kish KF, Kiefer SE, Sack JS, Newitt JA, Witmer MR, McKinnon M, Barrish JC, Dodd JH, Schieven GL, Leftheris K.
Bioorg Med Chem Lett (2013) 23 : 4120 -4126
PubMed 23746475 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.10 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL258202 1 8.70
CHEMBL2401979 1 8.40
CHEMBL1230065 BMS-582949 2.0 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL258202 IC50 = 2.0 nM 8.70
CHEMBL2401979 IC50 = 4.0 nM 8.40
CHEMBL1230065 BMS-582949 IC50 = 62.0 nM 7.21