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Assay Detail

CHEMBL2060772

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Binding
Inhibition of p38alpha
24
Total Activities
24
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 novel hedgehog antagonists from cell-based screening: Isosteric modification of p38 bisamides as potent inhibitors of SMO.
Yang B, Hird AW, Russell DJ, Fauber BP, Dakin LA, Zheng X, Su Q, Godin R, Brassil P, Devereaux E, Janetka JW.
Bioorg Med Chem Lett (2012) 22 : 4907 -4911
PubMed 22704236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.25 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183630 1 7.77
CHEMBL184712 1 7.60
CHEMBL184721 1 7.52
CHEMBL366255 1 7.29
CHEMBL365472 1 6.78
CHEMBL2059860 1 5.80
CHEMBL2059865 1 5.57
CHEMBL2057337 1 5.46
CHEMBL2059864 1 5.23
CHEMBL2059863 1 4.92
CHEMBL2059873 1 4.85
CHEMBL2059875 1 4.82
CHEMBL2057336 1 4.82
CHEMBL2059861 1 4.82
CHEMBL2059866 1 4.72
CHEMBL2059876 1 4.66
CHEMBL2059872 1 4.52
CHEMBL2059859 1 4.52
CHEMBL2059867 1 4.44
CHEMBL2059862 1 4.00
CHEMBL2059868 1 4.00
CHEMBL2059869 1 4.00
CHEMBL2059870 1 4.00
CHEMBL2059871 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183630 IC50 = 17.0 nM 7.77
CHEMBL184712 IC50 = 25.0 nM 7.60
CHEMBL184721 IC50 = 30.0 nM 7.52
CHEMBL366255 IC50 = 51.0 nM 7.29
CHEMBL365472 IC50 = 166.0 nM 6.78
CHEMBL2059860 IC50 = 1600.0 nM 5.80
CHEMBL2059865 IC50 = 2700.0 nM 5.57
CHEMBL2057337 IC50 = 3500.0 nM 5.46
CHEMBL2059864 IC50 = 5900.0 nM 5.23
CHEMBL2059863 IC50 = 12000.0 nM 4.92
CHEMBL2059873 IC50 = 14000.0 nM 4.85
CHEMBL2059875 IC50 = 15000.0 nM 4.82
CHEMBL2057336 IC50 = 15000.0 nM 4.82
CHEMBL2059861 IC50 = 15000.0 nM 4.82
CHEMBL2059866 IC50 = 19000.0 nM 4.72
CHEMBL2059876 IC50 = 22000.0 nM 4.66
CHEMBL2059872 IC50 = 30000.0 nM 4.52
CHEMBL2059859 IC50 = 30000.0 nM 4.52
CHEMBL2059867 IC50 = 36000.0 nM 4.44
CHEMBL2059862 IC50 = 100000.0 nM 4.00
CHEMBL2059868 IC50 = 100000.0 nM 4.00
CHEMBL2059869 IC50 = 100000.0 nM 4.00
CHEMBL2059870 IC50 = 100000.0 nM 4.00
CHEMBL2059871 IC50 = 100000.0 nM 4.00