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Assay Detail

CHEMBL2090336

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

Binding
Inhibition of mouse p38apha assessed as reduction in GST-ATF2 substrate phosphorylation by SPA assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 14 (CHEMBL2336)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis and biological activity of pyridopyridazin-6-one p38α MAP kinase inhibitors. Part 2.
Tynebor RM, Chen MH, Natarajan SR, O'Neill EA, Thompson JE, Fitzgerald CE, O'Keefe SJ, Doherty JB.
Bioorg Med Chem Lett (2012) 22 : 5979 -5983
PubMed 22901390 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 8.35 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2088591 1 9.48
CHEMBL2088578 1 9.24
CHEMBL2088588 1 9.24
CHEMBL2088582 1 8.89
CHEMBL2088590 1 8.80
CHEMBL2088589 1 8.80
CHEMBL2088583 1 8.64
CHEMBL2088575 1 8.64
CHEMBL2088579 1 8.48
CHEMBL2088586 1 8.33
CHEMBL2088576 1 8.24
CHEMBL1098524 1 8.15
CHEMBL2088587 1 8.06
CHEMBL2088580 1 8.05
CHEMBL2088577 1 8.00
CHEMBL1096192 1 7.89
CHEMBL1098546 1 7.85
CHEMBL2088585 1 7.77
CHEMBL2088584 1 7.50
CHEMBL2088581 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2088591 IC50 = 0.33 nM 9.48
CHEMBL2088578 IC50 = 0.58 nM 9.24
CHEMBL2088588 IC50 = 0.58 nM 9.24
CHEMBL2088582 IC50 = 1.3 nM 8.89
CHEMBL2088590 IC50 = 1.6 nM 8.80
CHEMBL2088589 IC50 = 1.6 nM 8.80
CHEMBL2088583 IC50 = 2.3 nM 8.64
CHEMBL2088575 IC50 = 2.3 nM 8.64
CHEMBL2088579 IC50 = 3.3 nM 8.48
CHEMBL2088586 IC50 = 4.7 nM 8.33
CHEMBL2088576 IC50 = 5.8 nM 8.24
CHEMBL1098524 IC50 = 7.1 nM 8.15
CHEMBL2088587 IC50 = 8.8 nM 8.06
CHEMBL2088580 IC50 = 9.0 nM 8.05
CHEMBL2088577 IC50 = 9.9 nM 8.00
CHEMBL1096192 IC50 = 13.0 nM 7.89
CHEMBL1098546 IC50 = 14.0 nM 7.85
CHEMBL2088585 IC50 = 17.0 nM 7.77
CHEMBL2088584 IC50 = 32.0 nM 7.50
CHEMBL2088581 IC50 = 99.0 nM 7.00