Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1932272

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

Binding
Inhibition of p38alpha assessed as [33P]gamma-ATP incorporation into GST-ATF2 substrate preincubated for 20 mins before substrate addition measured after 70 mins by liquid scintillation counter
ChEMBL ↗
46
Total Activities
46
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

Discovery of a novel class of non-ATP site DFG-out state p38 inhibitors utilizing computationally assisted virtual fragment-based drug design (vFBDD).
Moffett K, Konteatis Z, Nguyen D, Shetty R, Ludington J, Fujimoto T, Lee KJ, Chai X, Namboodiri H, Karpusas M, Dorsey B, Guarnieri F, Bukhtiyarova M, Springman E, Michelotti E.
Bioorg Med Chem Lett (2011) 21 : 7155 -7165
PubMed 22014550 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.92 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1929230 — — 1 8.70
CHEMBL1929224 — — 1 8.22
CHEMBL1926710 — — 1 8.00
CHEMBL1929216 — — 1 7.92
CHEMBL1929222 — — 1 7.92
CHEMBL1929226 — — 1 7.89
CHEMBL1929233 — — 1 7.89
CHEMBL1929231 — — 1 7.85
CHEMBL1929219 — — 1 7.75
CHEMBL1929215 — — 1 7.75
CHEMBL1929235 — — 1 7.72
CHEMBL1929227 — — 1 7.66
CHEMBL1929238 — — 1 7.66
CHEMBL1929221 — — 1 7.60
CHEMBL1929236 — — 1 7.54
CHEMBL1929217 — — 1 7.52
CHEMBL1929234 — — 1 7.51
CHEMBL1929237 — — 1 7.41
CHEMBL1929225 — — 1 7.38
CHEMBL1929239 — — 1 7.14
CHEMBL1929195 — — 1 7.12
CHEMBL1929228 — — 1 7.10
CHEMBL1929220 — — 1 7.08
CHEMBL1929223 — — 1 7.07
CHEMBL1929218 — — 1 6.96
CHEMBL1929196 — — 1 6.96
CHEMBL1929202 — — 1 6.92
CHEMBL1929229 — — 1 6.89
CHEMBL1929201 — — 1 6.89
CHEMBL1929232 — — 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1929230 — IC50 = 2.0 nM 8.70
CHEMBL1929224 — IC50 = 6.0 nM 8.22
CHEMBL1926710 — IC50 = 10.0 nM 8.00
CHEMBL1929216 — IC50 = 12.0 nM 7.92
CHEMBL1929222 — IC50 = 12.0 nM 7.92
CHEMBL1929226 — IC50 = 13.0 nM 7.89
CHEMBL1929233 — IC50 = 13.0 nM 7.89
CHEMBL1929231 — IC50 = 14.0 nM 7.85
CHEMBL1929219 — IC50 = 18.0 nM 7.75
CHEMBL1929215 — IC50 = 18.0 nM 7.75
CHEMBL1929235 — IC50 = 19.0 nM 7.72
CHEMBL1929227 — IC50 = 22.0 nM 7.66
CHEMBL1929238 — IC50 = 22.0 nM 7.66
CHEMBL1929221 — IC50 = 25.0 nM 7.60
CHEMBL1929236 — IC50 = 29.0 nM 7.54
CHEMBL1929217 — IC50 = 30.0 nM 7.52
CHEMBL1929234 — IC50 = 31.0 nM 7.51
CHEMBL1929237 — IC50 = 39.0 nM 7.41
CHEMBL1929225 — IC50 = 42.0 nM 7.38
CHEMBL1929239 — IC50 = 73.0 nM 7.14
CHEMBL1929195 — IC50 = 76.0 nM 7.12
CHEMBL1929228 — IC50 = 80.0 nM 7.10
CHEMBL1929220 — IC50 = 83.0 nM 7.08
CHEMBL1929223 — IC50 = 86.0 nM 7.07
CHEMBL1929196 — IC50 = 110.0 nM 6.96
CHEMBL1929218 — IC50 = 110.0 nM 6.96
CHEMBL1929202 — IC50 = 120.0 nM 6.92
CHEMBL1929229 — IC50 = 130.0 nM 6.89
CHEMBL1929201 — IC50 = 130.0 nM 6.89
CHEMBL1929232 — IC50 = 140.0 nM 6.85
CHEMBL1929198 — IC50 = 220.0 nM 6.66
CHEMBL1929203 — IC50 = 240.0 nM 6.62
CHEMBL1929197 — IC50 = 250.0 nM 6.60
CHEMBL1929207 — IC50 = 520.0 nM 6.28
CHEMBL1929199 — IC50 = 900.0 nM 6.05
CHEMBL1929204 — IC50 = 1200.0 nM 5.92
CHEMBL1929200 — IC50 = 1700.0 nM 5.77
CHEMBL1929208 — IC50 = 2000.0 nM 5.70
CHEMBL1929214 — IC50 = 2000.0 nM 5.70
CHEMBL1929210 — IC50 = 2300.0 nM 5.64
CHEMBL1929211 — IC50 = 3500.0 nM 5.46
CHEMBL1929205 — IC50 = 5700.0 nM 5.24
CHEMBL1929209 — IC50 = 6400.0 nM 5.19
CHEMBL1929212 — IC50 = 10000.0 nM 5.00
CHEMBL1929206 — IC50 = 16000.0 nM 4.80
CHEMBL1929213 — IC50 > 10000.0 nM -