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Assay Detail

CHEMBL5167053

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

Binding
Inhibition of human recombinant full length GST-tagged p38alpha expressed in Escherichia coli preincubated for 2 hrs followed by ATP addition and measured after 1 hr by Alpha screen assay
ChEMBL ↗
43
Total Activities
43
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

Design, Synthesis, and Biological Characterization of Inhaled p38α/β MAPK Inhibitors for the Treatment of Lung Inflammatory Diseases.
Armani E, Capaldi C, Bagnacani V, Saccani F, Aquino G, Puccini P, Facchinetti F, Martucci C, Moretto N, Villetti G, Patacchini R, Civelli M, Hurley C, Jennings A, Alcaraz L, Bloomfield D, Briggs M, Daly S, Panchal T, Russell V, Wicks S, Finch H, Fitzgerald M, Fox C, Delcanale M.
J Med Chem (2022) 65 : 7170 -7192
PubMed 35546685 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 43 9.51 10.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5186216 — — 1 10.52
CHEMBL5172781 — — 1 10.30
CHEMBL5174953 — — 1 10.30
CHEMBL5180443 — — 1 10.22
CHEMBL5206397 — — 1 10.10
CHEMBL5173417 — — 1 10.00
CHEMBL5200224 — — 1 10.00
CHEMBL5202475 — — 1 10.00
CHEMBL5198434 — — 1 9.70
CHEMBL5206328 — — 1 9.70
CHEMBL5207849 — — 1 9.70
CHEMBL5203796 — — 1 9.70
CHEMBL5208103 — — 1 9.70
CHEMBL5198371 — — 1 9.70
CHEMBL5190010 — — 1 9.70
CHEMBL5197888 — — 1 9.52
CHEMBL5198646 — — 1 9.52
CHEMBL5194894 — — 1 9.52
CHEMBL5190292 — — 1 9.52
CHEMBL5184542 — — 1 9.52
CHEMBL5189475 — — 1 9.52
CHEMBL5176351 — — 1 9.52
CHEMBL5198204 — — 1 9.52
CHEMBL5186620 — — 1 9.52
CHEMBL5195994 — — 1 9.40
CHEMBL5177395 — — 1 9.40
CHEMBL5193720 — — 1 9.40
CHEMBL5202281 — — 1 9.40
CHEMBL5203029 — — 1 9.30
CHEMBL5202884 — — 1 9.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5186216 — IC50 = 0.03 nM 10.52
CHEMBL5172781 — IC50 = 0.05 nM 10.30
CHEMBL5174953 — IC50 = 0.05 nM 10.30
CHEMBL5180443 — IC50 = 0.06 nM 10.22
CHEMBL5206397 — IC50 = 0.08 nM 10.10
CHEMBL5173417 — IC50 = 0.1 nM 10.00
CHEMBL5200224 — IC50 = 0.1 nM 10.00
CHEMBL5202475 — IC50 = 0.1 nM 10.00
CHEMBL5198371 — IC50 = 0.2 nM 9.70
CHEMBL5206328 — IC50 = 0.2 nM 9.70
CHEMBL5207849 — IC50 = 0.2 nM 9.70
CHEMBL5203796 — IC50 = 0.2 nM 9.70
CHEMBL5208103 — IC50 = 0.2 nM 9.70
CHEMBL5198434 — IC50 = 0.2 nM 9.70
CHEMBL5190010 — IC50 = 0.2 nM 9.70
CHEMBL5190292 — IC50 = 0.3 nM 9.52
CHEMBL5198646 — IC50 = 0.3 nM 9.52
CHEMBL5194894 — IC50 = 0.3 nM 9.52
CHEMBL5184542 — IC50 = 0.3 nM 9.52
CHEMBL5176351 — IC50 = 0.3 nM 9.52
CHEMBL5198204 — IC50 = 0.3 nM 9.52
CHEMBL5186620 — IC50 = 0.3 nM 9.52
CHEMBL5197888 — IC50 = 0.3 nM 9.52
CHEMBL5189475 — IC50 = 0.3 nM 9.52
CHEMBL5195994 — IC50 = 0.4 nM 9.40
CHEMBL5177395 — IC50 = 0.4 nM 9.40
CHEMBL5193720 — IC50 = 0.4 nM 9.40
CHEMBL5202281 — IC50 = 0.4 nM 9.40
CHEMBL5202397 — IC50 = 0.5 nM 9.30
CHEMBL5169767 — IC50 = 0.5 nM 9.30
CHEMBL5201578 — IC50 = 0.5 nM 9.30
CHEMBL5202884 — IC50 = 0.5 nM 9.30
CHEMBL5203029 — IC50 = 0.5 nM 9.30
CHEMBL5185806 — IC50 = 0.6 nM 9.22
CHEMBL5183262 — IC50 = 0.6 nM 9.22
CHEMBL5174266 — IC50 = 0.6 nM 9.22
CHEMBL5197124 — IC50 = 0.8 nM 9.10
CHEMBL5207264 — IC50 = 0.8 nM 9.10
CHEMBL5205402 — IC50 = 1.0 nM 9.00
CHEMBL5208101 — IC50 = 1.1 nM 8.96
CHEMBL5175094 — IC50 = 1.3 nM 8.89
CHEMBL5185814 — IC50 = 2.0 nM 8.70
CHEMBL5204479 — IC50 = 6.1 nM 8.21