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Assay Detail

CHEMBL734090

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

Binding
Inhibitory activity against mitogen-activated protein kinase p38 alpha
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Mitogen-activated protein kinase 14 (CHEMBL260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of potent, orally bioavailable dihydroquinazolinone inhibitors of p38 MAP kinase.
Stelmach JE, Liu L, Patel SB, Pivnichny JV, Scapin G, Singh S, Hop CE, Wang Z, Strauss JR, Cameron PM, Nichols EA, O'Keefe SJ, O'Neill EA, Schmatz DM, Schwartz CD, Thompson CM, Zaller DM, Doherty JB.
Bioorg Med Chem Lett (2003) 13 : 277 -280
PubMed 12482439 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 8.58 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL97227 1 10.00
CHEMBL328614 1 10.00
CHEMBL327959 1 10.00
CHEMBL327746 1 9.89
CHEMBL316604 1 9.70
CHEMBL94825 1 9.70
CHEMBL319556 1 9.70
CHEMBL318934 1 9.52
CHEMBL419140 1 9.40
CHEMBL327987 1 9.30
CHEMBL96653 1 9.30
CHEMBL419134 1 9.30
CHEMBL328242 1 9.22
CHEMBL96432 1 9.22
CHEMBL264627 1 9.22
CHEMBL96763 1 9.05
CHEMBL94556 1 9.00
CHEMBL96565 1 8.96
CHEMBL96225 1 8.96
CHEMBL96345 1 8.92
CHEMBL96487 1 8.85
CHEMBL94444 1 8.82
CHEMBL327217 1 8.62
CHEMBL94417 1 8.59
CHEMBL94770 1 8.52
CHEMBL96632 1 8.22
CHEMBL94547 1 8.15
CHEMBL94495 1 8.15
CHEMBL96091 1 7.96
CHEMBL94783 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL97227 IC50 = 0.1 nM 10.00
CHEMBL327959 IC50 = 0.1 nM 10.00
CHEMBL328614 IC50 = 0.1 nM 10.00
CHEMBL327746 IC50 = 0.13 nM 9.89
CHEMBL316604 IC50 = 0.2 nM 9.70
CHEMBL94825 IC50 = 0.2 nM 9.70
CHEMBL319556 IC50 = 0.2 nM 9.70
CHEMBL318934 IC50 = 0.3 nM 9.52
CHEMBL419140 IC50 = 0.4 nM 9.40
CHEMBL419134 IC50 = 0.5 nM 9.30
CHEMBL96653 IC50 = 0.5 nM 9.30
CHEMBL327987 IC50 = 0.5 nM 9.30
CHEMBL328242 IC50 = 0.6 nM 9.22
CHEMBL96432 IC50 = 0.6 nM 9.22
CHEMBL264627 IC50 = 0.6 nM 9.22
CHEMBL96763 IC50 = 0.9 nM 9.05
CHEMBL94556 IC50 = 1.0 nM 9.00
CHEMBL96565 IC50 = 1.1 nM 8.96
CHEMBL96225 IC50 = 1.1 nM 8.96
CHEMBL96345 IC50 = 1.2 nM 8.92
CHEMBL96487 IC50 = 1.4 nM 8.85
CHEMBL94444 IC50 = 1.5 nM 8.82
CHEMBL327217 IC50 = 2.4 nM 8.62
CHEMBL94417 IC50 = 2.6 nM 8.59
CHEMBL94770 IC50 = 3.0 nM 8.52
CHEMBL96632 IC50 = 6.0 nM 8.22
CHEMBL94547 IC50 = 7.0 nM 8.15
CHEMBL94495 IC50 = 7.0 nM 8.15
CHEMBL96091 IC50 = 11.0 nM 7.96
CHEMBL94783 IC50 = 11.0 nM 7.96
CHEMBL94377 IC50 = 11.0 nM 7.96
CHEMBL328252 IC50 = 22.0 nM 7.66
CHEMBL421194 IC50 = 30.0 nM 7.52
CHEMBL97579 IC50 = 44.0 nM 7.36
CHEMBL316337 IC50 = 44.0 nM 7.36
CHEMBL330358 IC50 = 47.0 nM 7.33
CHEMBL421566 IC50 = 67.0 nM 7.17
CHEMBL94852 IC50 = 79.0 nM 7.10
CHEMBL94719 IC50 = 130.0 nM 6.89
CHEMBL328752 IC50 = 170.0 nM 6.77
CHEMBL328274 IC50 = 320.0 nM 6.50