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Assay Detail

CHEMBL732636

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Binding
Inhibitory activity against Mitogen-activated protein kinase p38 (MAP kinase)
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

MAP kinase p38 (CHEMBL2094115)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Design and synthesis of potent, selective, and orally bioavailable tetrasubstituted imidazole inhibitors of p38 mitogen-activated protein kinase.
Liverton NJ, Butcher JW, Claiborne CF, Claremon DA, Libby BE, Nguyen KT, Pitzenberger SM, Selnick HG, Smith GR, Tebben A, Vacca JP, Varga SL, Agarwal L, Dancheck K, Forsyth AJ, Fletcher DS, Frantz B, Hanlon WA, Harper CF, Hofsess SJ, Kostura M, Lin J, Luell S, O'Neill EA, O'Keefe SJ.
J Med Chem (1999) 42 : 2180 -2190
PubMed 10377223 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.91 9.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446404 1 9.01
CHEMBL307435 1 8.82
CHEMBL69764 1 8.05
CHEMBL67874 1 7.72
CHEMBL69929 1 7.55
CHEMBL68572 1 7.42
CHEMBL430419 1 7.32
CHEMBL302728 1 7.24
CHEMBL69331 1 7.16
CHEMBL67633 1 6.92
CHEMBL401695 1 6.89
CHEMBL70286 1 6.86
CHEMBL304624 1 6.85
CHEMBL404842 1 6.82
CHEMBL63135 1 6.77
CHEMBL69228 1 6.75
CHEMBL304166 1 6.70
CHEMBL402426 1 6.52
CHEMBL71955 1 6.30
CHEMBL305023 1 6.26
CHEMBL302805 1 6.16
CHEMBL307340 1 6.01
CHEMBL71987 1 6.00
CHEMBL305749 1 5.91
CHEMBL68215 1 5.85
CHEMBL71922 1 5.68
CHEMBL71403 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446404 IC50 = 0.97 nM 9.01
CHEMBL307435 IC50 = 1.5 nM 8.82
CHEMBL69764 IC50 = 9.0 nM 8.05
CHEMBL67874 IC50 = 19.0 nM 7.72
CHEMBL69929 IC50 = 28.0 nM 7.55
CHEMBL68572 IC50 = 38.0 nM 7.42
CHEMBL430419 IC50 = 48.0 nM 7.32
CHEMBL302728 IC50 = 57.0 nM 7.24
CHEMBL69331 IC50 = 70.0 nM 7.16
CHEMBL67633 IC50 = 120.0 nM 6.92
CHEMBL401695 IC50 = 130.0 nM 6.89
CHEMBL70286 IC50 = 137.0 nM 6.86
CHEMBL304624 IC50 = 140.0 nM 6.85
CHEMBL404842 IC50 = 150.0 nM 6.82
CHEMBL63135 IC50 = 170.0 nM 6.77
CHEMBL69228 IC50 = 180.0 nM 6.75
CHEMBL304166 IC50 = 200.0 nM 6.70
CHEMBL402426 IC50 = 300.0 nM 6.52
CHEMBL71955 IC50 = 495.0 nM 6.30
CHEMBL305023 IC50 = 550.0 nM 6.26
CHEMBL302805 IC50 = 700.0 nM 6.16
CHEMBL307340 IC50 = 970.0 nM 6.01
CHEMBL71987 IC50 = 1000.0 nM 6.00
CHEMBL305749 IC50 = 1220.0 nM 5.91
CHEMBL68215 IC50 = 1400.0 nM 5.85
CHEMBL71922 IC50 = 2100.0 nM 5.68
CHEMBL71403 IC50 > 10000.0 nM -