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Assay Detail

CHEMBL4337359

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Binding
Inhibition of P38alpha MAPK (unknown origin)
32
Total Activities
26
Compounds Tested
2
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 potent p38α MAPK inhibitors through a funnel like workflow combining in silico screening and in vitro validation.
Astolfi A, Kudolo M, Brea J, Manni G, Manfroni G, Palazzotti D, Sabatini S, Cecchetti F, Felicetti T, Cannalire R, Massari S, Tabarrini O, Loza MI, Fallarino F, Cecchetti V, Laufer SA, Barreca ML.
Eur J Med Chem (2019) 182 : 111624 -111624
PubMed 31445234 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 8.09 9.10
Ki 8 7.99 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492265 2 9.40
CHEMBL1232751 1 9.05
CHEMBL494072 1 9.05
CHEMBL4575052 1 9.00
CHEMBL1082158 2 9.00
CHEMBL3086685 1 9.00
CHEMBL1800911 1 8.89
CHEMBL252535 1 8.66
CHEMBL1091199 1 8.64
CHEMBL1234931 1 8.52
CHEMBL252128 1 8.51
CHEMBL559401 1 8.49
CHEMBL258202 1 8.46
CHEMBL1230070 1 8.41
CHEMBL1807446 1 8.40
CHEMBL4593539 1 8.15
CHEMBL2401978 1 8.15
CHEMBL1232887 2 8.05
CHEMBL522579 1 8.00
CHEMBL4535046 1 8.00
CHEMBL478649 2 7.92
CHEMBL1230065 BMS-582949 2.0 1 7.89
CHEMBL2177219 1 7.46
CHEMBL1938764 1 7.24
CHEMBL270164 GW607117X 2 6.62
CHEMBL273158 2 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492265 Ki = 0.4 nM 9.40
CHEMBL492265 IC50 = 0.8 nM 9.10
CHEMBL494072 IC50 = 0.9 nM 9.05
CHEMBL1232751 IC50 = 0.9 nM 9.05
CHEMBL4575052 IC50 = 1.0 nM 9.00
CHEMBL1082158 Ki = 1.0 nM 9.00
CHEMBL3086685 IC50 = 1.0 nM 9.00
CHEMBL1800911 IC50 = 1.3 nM 8.89
CHEMBL1082158 IC50 = 1.4 nM 8.85
CHEMBL252535 IC50 = 2.2 nM 8.66
CHEMBL1091199 Ki = 2.3 nM 8.64
CHEMBL1234931 IC50 = 3.0 nM 8.52
CHEMBL252128 IC50 = 3.1 nM 8.51
CHEMBL559401 IC50 = 3.2 nM 8.49
CHEMBL258202 IC50 = 3.5 nM 8.46
CHEMBL1230070 IC50 = 3.9 nM 8.41
CHEMBL1807446 IC50 = 4.0 nM 8.40
CHEMBL2401978 IC50 = 7.0 nM 8.15
CHEMBL4593539 IC50 = 7.0 nM 8.15
CHEMBL1232887 Ki = 9.0 nM 8.05
CHEMBL522579 Ki = 10.0 nM 8.00
CHEMBL4535046 IC50 = 10.0 nM 8.00
CHEMBL478649 Ki = 12.0 nM 7.92
CHEMBL1230065 BMS-582949 IC50 = 13.0 nM 7.89
CHEMBL2177219 IC50 = 35.0 nM 7.46
CHEMBL1938764 IC50 = 58.0 nM 7.24
CHEMBL478649 IC50 = 75.0 nM 7.12
CHEMBL270164 GW607117X Ki = 240.0 nM 6.62
CHEMBL1232887 IC50 = 316.2 nM 6.50
CHEMBL273158 Ki = 480.0 nM 6.32
CHEMBL270164 GW607117X IC50 = 1500.0 nM 5.82
CHEMBL273158 IC50 = 3000.0 nM 5.52