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Assay Detail

CHEMBL3123036

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Binding
Inhibition of p38a MAPK (unknown origin) by radiometric assay
ChEMBL ↗
54
Total Activities
54
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

Syntheses and structure-activity relationships for some triazolyl p38α MAPK inhibitors.
Seerden JP, Leusink-Ionescu G, Leguijt R, Saccavini C, Gelens E, Dros B, Woudenberg-Vrenken T, Molema G, Kamps JA, Kellogg RM.
Bioorg Med Chem Lett (2014) 24 : 1352 -1357
PubMed 24508134 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 54 5.96 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3120970 — — 1 8.22
CHEMBL10 SB-203580 — 1 7.40
CHEMBL3120173 — — 1 7.04
CHEMBL3120986 — — 1 7.02
CHEMBL3120995 — — 1 6.85
CHEMBL3120960 — — 1 6.85
CHEMBL3120983 — — 1 6.73
CHEMBL3120996 — — 1 6.72
CHEMBL3120984 — — 1 6.60
CHEMBL3120987 — — 1 6.54
CHEMBL3120985 — — 1 6.46
CHEMBL3120961 — — 1 6.42
CHEMBL3120975 — — 1 6.40
CHEMBL3120980 — — 1 6.37
CHEMBL3120971 — — 1 6.37
CHEMBL3120974 — — 1 6.34
CHEMBL3120963 — — 1 6.30
CHEMBL3120977 — — 1 6.23
CHEMBL366007 — — 1 6.22
CHEMBL3121004 — — 1 6.15
CHEMBL3120972 — — 1 6.14
CHEMBL3120979 — — 1 6.13
CHEMBL3120988 — — 1 6.05
CHEMBL3120997 — — 1 6.00
CHEMBL3120978 — — 1 5.93
CHEMBL3121005 — — 1 5.92
CHEMBL3120993 — — 1 5.85
CHEMBL3120966 — — 1 5.84
CHEMBL3120968 — — 1 5.83
CHEMBL3120998 — — 1 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3120970 — IC50 = 6.0 nM 8.22
CHEMBL10 SB-203580 IC50 = 40.0 nM 7.40
CHEMBL3120173 — IC50 = 91.0 nM 7.04
CHEMBL3120986 — IC50 = 96.0 nM 7.02
CHEMBL3120995 — IC50 = 140.0 nM 6.85
CHEMBL3120960 — IC50 = 140.0 nM 6.85
CHEMBL3120983 — IC50 = 185.0 nM 6.73
CHEMBL3120996 — IC50 = 190.0 nM 6.72
CHEMBL3120984 — IC50 = 250.0 nM 6.60
CHEMBL3120987 — IC50 = 290.0 nM 6.54
CHEMBL3120985 — IC50 = 350.0 nM 6.46
CHEMBL3120961 — IC50 = 380.0 nM 6.42
CHEMBL3120975 — IC50 = 400.0 nM 6.40
CHEMBL3120971 — IC50 = 430.0 nM 6.37
CHEMBL3120980 — IC50 = 430.0 nM 6.37
CHEMBL3120974 — IC50 = 460.0 nM 6.34
CHEMBL3120963 — IC50 = 500.0 nM 6.30
CHEMBL3120977 — IC50 = 590.0 nM 6.23
CHEMBL366007 — IC50 = 600.0 nM 6.22
CHEMBL3121004 — IC50 = 710.0 nM 6.15
CHEMBL3120972 — IC50 = 730.0 nM 6.14
CHEMBL3120979 — IC50 = 740.0 nM 6.13
CHEMBL3120988 — IC50 = 890.0 nM 6.05
CHEMBL3120997 — IC50 = 990.0 nM 6.00
CHEMBL3120978 — IC50 = 1170.0 nM 5.93
CHEMBL3121005 — IC50 = 1190.0 nM 5.92
CHEMBL3120993 — IC50 = 1400.0 nM 5.85
CHEMBL3120966 — IC50 = 1440.0 nM 5.84
CHEMBL3120968 — IC50 = 1490.0 nM 5.83
CHEMBL3120998 — IC50 = 1530.0 nM 5.82
CHEMBL3121000 — IC50 = 1590.0 nM 5.80
CHEMBL3120973 — IC50 = 1790.0 nM 5.75
CHEMBL3120964 — IC50 = 1870.0 nM 5.73
CHEMBL3121001 — IC50 = 2170.0 nM 5.66
CHEMBL3120982 — IC50 = 2300.0 nM 5.64
CHEMBL3120989 — IC50 = 2400.0 nM 5.62
CHEMBL3120981 — IC50 = 3200.0 nM 5.50
CHEMBL3120990 — IC50 = 3800.0 nM 5.42
CHEMBL3120992 — IC50 = 4200.0 nM 5.38
CHEMBL3121006 — IC50 = 5180.0 nM 5.29
CHEMBL3120976 — IC50 = 5730.0 nM 5.24
CHEMBL3120999 — IC50 = 6510.0 nM 5.19
CHEMBL3121007 — IC50 = 11200.0 nM 4.95
CHEMBL3121009 — IC50 = 11600.0 nM 4.94
CHEMBL3120967 — IC50 = 11400.0 nM 4.94
CHEMBL3121008 — IC50 = 12500.0 nM 4.90
CHEMBL3120994 — IC50 = 19500.0 nM 4.71
CHEMBL3120959 — IC50 = 23500.0 nM 4.63
CHEMBL3120991 — IC50 = 56000.0 nM 4.25
CHEMBL3121002 — IC50 > 100000.0 nM -