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Assay Detail

CHEMBL2184768

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Binding
Inhibition of MAP kinase p38alpha assessed as phosphorylation of ATF-2
ChEMBL ↗
69
Total Activities
69
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 14 (CHEMBL260) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting the hinge glycine flip and the activation loop: novel approach to potent p38α inhibitors.
Martz KE, Dorn A, Baur B, Schattel V, Goettert MI, Mayer-Wrangowski SC, Rauh D, Laufer SA.
J Med Chem (2012) 55 : 7862 -7874
PubMed 22897496 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 69 6.97 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2182085 — — 1 8.52
CHEMBL2182072 — — 1 8.40
CHEMBL2177215 — — 1 8.30
CHEMBL2182071 — — 1 8.05
CHEMBL2182089 — — 1 8.00
CHEMBL2182074 — — 1 8.00
CHEMBL2177214 — — 1 8.00
CHEMBL2182088 — — 1 7.96
CHEMBL2182090 — — 1 7.92
CHEMBL2177106 — — 1 7.92
CHEMBL2182082 — — 1 7.92
CHEMBL2182099 — — 1 7.89
CHEMBL2177213 — — 1 7.85
CHEMBL2177217 — — 1 7.85
CHEMBL2177209 — — 1 7.82
CHEMBL2177221 — — 1 7.77
CHEMBL2182084 — — 1 7.77
CHEMBL2182087 — — 1 7.70
CHEMBL2177224 — — 1 7.70
CHEMBL2177222 — — 1 7.62
CHEMBL2177223 — — 1 7.60
CHEMBL2182070 — — 1 7.57
CHEMBL2182083 — — 1 7.57
CHEMBL2182073 — — 1 7.54
CHEMBL2182067 — — 1 7.52
CHEMBL2182081 — — 1 7.50
CHEMBL2177219 — — 1 7.46
CHEMBL2177212 — — 1 7.46
CHEMBL2177211 — — 1 7.44
CHEMBL2177216 — — 1 7.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2182085 — IC50 = 3.0 nM 8.52
CHEMBL2182072 — IC50 = 4.0 nM 8.40
CHEMBL2177215 — IC50 = 5.0 nM 8.30
CHEMBL2182071 — IC50 = 9.0 nM 8.05
CHEMBL2182089 — IC50 = 10.0 nM 8.00
CHEMBL2182074 — IC50 = 10.0 nM 8.00
CHEMBL2177214 — IC50 = 10.0 nM 8.00
CHEMBL2182088 — IC50 = 11.0 nM 7.96
CHEMBL2182090 — IC50 = 12.0 nM 7.92
CHEMBL2177106 — IC50 = 12.0 nM 7.92
CHEMBL2182082 — IC50 = 12.0 nM 7.92
CHEMBL2182099 — IC50 = 13.0 nM 7.89
CHEMBL2177213 — IC50 = 14.0 nM 7.85
CHEMBL2177217 — IC50 = 14.0 nM 7.85
CHEMBL2177209 — IC50 = 15.0 nM 7.82
CHEMBL2177221 — IC50 = 17.0 nM 7.77
CHEMBL2182084 — IC50 = 17.0 nM 7.77
CHEMBL2182087 — IC50 = 20.0 nM 7.70
CHEMBL2177224 — IC50 = 20.0 nM 7.70
CHEMBL2177222 — IC50 = 24.0 nM 7.62
CHEMBL2177223 — IC50 = 25.0 nM 7.60
CHEMBL2182070 — IC50 = 27.0 nM 7.57
CHEMBL2182083 — IC50 = 27.0 nM 7.57
CHEMBL2182073 — IC50 = 29.0 nM 7.54
CHEMBL2182067 — IC50 = 30.0 nM 7.52
CHEMBL2182081 — IC50 = 32.0 nM 7.50
CHEMBL2177212 — IC50 = 35.0 nM 7.46
CHEMBL2177219 — IC50 = 35.0 nM 7.46
CHEMBL2177211 — IC50 = 36.0 nM 7.44
CHEMBL2177216 — IC50 = 37.0 nM 7.43
CHEMBL10 SB-203580 IC50 = 37.0 nM 7.43
CHEMBL2177205 — IC50 = 40.0 nM 7.40
CHEMBL2182086 — IC50 = 40.0 nM 7.40
CHEMBL2182101 — IC50 = 40.0 nM 7.40
CHEMBL2182103 — IC50 = 42.0 nM 7.38
CHEMBL218962 — IC50 = 50.0 nM 7.30
CHEMBL2177220 — IC50 = 55.0 nM 7.26
CHEMBL2182069 — IC50 = 83.0 nM 7.08
CHEMBL2182110 — IC50 = 84.0 nM 7.08
CHEMBL2182094 — IC50 = 100.0 nM 7.00
CHEMBL2177218 — IC50 = 120.0 nM 6.92
CHEMBL2177206 — IC50 = 130.0 nM 6.89
CHEMBL2177208 — IC50 = 130.0 nM 6.89
CHEMBL2182109 — IC50 = 160.0 nM 6.80
CHEMBL2177210 — IC50 = 180.0 nM 6.75
CHEMBL2177226 — IC50 = 200.0 nM 6.70
CHEMBL2177204 — IC50 = 210.0 nM 6.68
CHEMBL2182108 — IC50 = 220.0 nM 6.66
CHEMBL2182080 — IC50 = 220.0 nM 6.66
CHEMBL2182100 — IC50 = 300.0 nM 6.52