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Assay Detail

CHEMBL4822083

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Binding
Binding affinity to P38alpha MAPK (unknown origin) using Smad3 as substrate incubated for 1 hr in presence of ATP by ELISA based competitive binding potency assay
10
Total Activities
10
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

Identification of an allosteric and Smad3-selective inhibitor of p38αMAPK using a substrate-based approach.
Nagao H, Kitagawa D, Nakajima F, Sawa M, Kinoshita T.
Bioorg Med Chem Lett (2021) 43 : 128056 -128056
PubMed 33892104 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.76 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4868525 1 8.89
CHEMBL278041 SB-202190 1 7.96
CHEMBL4852110 1 6.54
CHEMBL4847239 1 6.52
CHEMBL4870695 1 5.58
CHEMBL4858673 1 5.05
CHEMBL4850724 1 -
CHEMBL4861772 1 -
CHEMBL4860774 1 -
CHEMBL4864686 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4868525 IC50 = 1.3 nM 8.89
CHEMBL278041 SB-202190 IC50 = 11.0 nM 7.96
CHEMBL4852110 IC50 = 290.0 nM 6.54
CHEMBL4847239 IC50 = 300.0 nM 6.52
CHEMBL4870695 IC50 = 2600.0 nM 5.58
CHEMBL4858673 IC50 = 9000.0 nM 5.05
CHEMBL4850724 IC50 > 100000.0 nM -
CHEMBL4861772 IC50 > 100000.0 nM -
CHEMBL4860774 IC50 > 100000.0 nM -
CHEMBL4864686 IC50 > 1000.0 nM -