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Assay Detail

CHEMBL3783189

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

Binding
Inhibition of human recombinant p38 alpha assessed as phosphorylation of MAPKAP-K2 preincubated for 2 hrs followed by FRET peptide and MAPKAP-K2 addition measured after 1 hr by Z-LYTE assay
30
Total Activities
30
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 14 (CHEMBL260)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Narrow Spectrum Kinase Inhibitors: New Therapeutic Agents for the Treatment of COPD and Steroid-Resistant Asthma.
Onions ST, Ito K, Charron CE, Brown RJ, Colucci M, Frickel F, Hardy G, Joly K, King-Underwood J, Kizawa Y, Knowles I, Murray PJ, Novak A, Rani A, Rapeport G, Smith A, Strong P, Taddei DM, Williams JG.
J Med Chem (2016) 59 : 1727 -1746
PubMed 26800309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.89 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3781244 1 9.00
CHEMBL3781102 1 8.70
CHEMBL3780667 1 8.70
CHEMBL3781245 1 8.70
CHEMBL3782036 1 8.52
CHEMBL3695568 JNJ-49095397 2.0 1 8.30
CHEMBL3781687 1 8.22
CHEMBL3781413 1 8.22
CHEMBL3782009 1 8.22
CHEMBL3780488 1 8.10
CHEMBL3780832 1 8.10
CHEMBL3781473 1 8.05
CHEMBL3781430 1 7.96
CHEMBL3780111 1 7.96
CHEMBL343227 1 7.92
CHEMBL3781532 1 7.89
CHEMBL143134 1 7.77
CHEMBL3780714 1 7.75
CHEMBL103667 DORAMAPIMOD 2.0 1 7.70
CHEMBL336001 1 7.66
CHEMBL3780519 1 7.62
CHEMBL3780629 1 7.60
CHEMBL3780386 1 7.57
CHEMBL3780154 1 7.51
CHEMBL3780089 1 7.48
CHEMBL3781999 1 7.42
CHEMBL3781982 1 7.28
CHEMBL3781587 1 7.22
CHEMBL3780410 1 6.91
CHEMBL3781528 1 6.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3781244 IC50 = 1.0 nM 9.00
CHEMBL3781102 IC50 = 2.0 nM 8.70
CHEMBL3780667 IC50 = 2.0 nM 8.70
CHEMBL3781245 IC50 = 2.0 nM 8.70
CHEMBL3782036 IC50 = 3.0 nM 8.52
CHEMBL3695568 JNJ-49095397 IC50 = 5.0 nM 8.30
CHEMBL3781687 IC50 = 6.0 nM 8.22
CHEMBL3781413 IC50 = 6.0 nM 8.22
CHEMBL3782009 IC50 = 6.0 nM 8.22
CHEMBL3780488 IC50 = 8.0 nM 8.10
CHEMBL3780832 IC50 = 8.0 nM 8.10
CHEMBL3781473 IC50 = 9.0 nM 8.05
CHEMBL3781430 IC50 = 11.0 nM 7.96
CHEMBL3780111 IC50 = 11.0 nM 7.96
CHEMBL343227 IC50 = 12.0 nM 7.92
CHEMBL3781532 IC50 = 13.0 nM 7.89
CHEMBL143134 IC50 = 17.0 nM 7.77
CHEMBL3780714 IC50 = 18.0 nM 7.75
CHEMBL103667 DORAMAPIMOD IC50 = 20.0 nM 7.70
CHEMBL336001 IC50 = 22.0 nM 7.66
CHEMBL3780519 IC50 = 24.0 nM 7.62
CHEMBL3780629 IC50 = 25.0 nM 7.60
CHEMBL3780386 IC50 = 27.0 nM 7.57
CHEMBL3780154 IC50 = 31.0 nM 7.51
CHEMBL3780089 IC50 = 33.0 nM 7.48
CHEMBL3781999 IC50 = 38.0 nM 7.42
CHEMBL3781982 IC50 = 52.0 nM 7.28
CHEMBL3781587 IC50 = 60.0 nM 7.22
CHEMBL3780410 IC50 = 123.0 nM 6.91
CHEMBL3781528 IC50 = 167.0 nM 6.78