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Assay Detail

CHEMBL734272

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Binding
Inhibitory activity against mitogen activated protein (MAP) kinase p38 alpha.
ChEMBL ↗
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Benzimidazolone p38 inhibitors.
Dombroski MA, Letavic MA, McClure KF, Barberia JT, Carty TJ, Cortina SR, Csiki C, Dipesa AJ, Elliott NC, Gabel CA, Jordan CK, Labasi JM, Martin WH, Peese KM, Stock IA, Svensson L, Sweeney FJ, Yu CH.
Bioorg Med Chem Lett (2004) 14 : 919 -923
PubMed 15012994 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 49 6.49 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303144 — — 1 8.70
CHEMBL355703 — — 1 8.05
CHEMBL353427 — — 1 7.52
CHEMBL10 SB-203580 — 1 7.42
CHEMBL95692 SB-242235 — 1 7.40
CHEMBL170631 — — 1 7.30
CHEMBL115769 — — 1 7.28
CHEMBL172689 — — 1 7.22
CHEMBL172286 — — 1 7.16
CHEMBL172232 — — 1 7.16
CHEMBL355790 — — 1 7.05
CHEMBL368200 — — 1 7.00
CHEMBL355529 — — 1 7.00
CHEMBL355528 — — 1 6.85
CHEMBL368345 — — 1 6.85
CHEMBL173857 — — 1 6.85
CHEMBL353440 — — 1 6.70
CHEMBL170830 — — 1 6.70
CHEMBL427114 — — 1 6.70
CHEMBL172882 — — 1 6.58
CHEMBL368455 — — 1 6.58
CHEMBL174257 — — 1 6.57
CHEMBL366533 — — 1 6.54
CHEMBL368397 — — 1 6.43
CHEMBL435669 — — 1 6.42
CHEMBL170535 — — 1 6.41
CHEMBL173908 — — 1 6.30
CHEMBL366605 — — 1 6.27
CHEMBL368543 — — 1 6.17
CHEMBL367111 — — 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303144 — IC50 = 2.0 nM 8.70
CHEMBL355703 — IC50 = 9.0 nM 8.05
CHEMBL353427 — IC50 = 30.0 nM 7.52
CHEMBL10 SB-203580 IC50 = 38.0 nM 7.42
CHEMBL95692 SB-242235 IC50 = 40.0 nM 7.40
CHEMBL170631 — IC50 = 50.0 nM 7.30
CHEMBL115769 — IC50 = 52.0 nM 7.28
CHEMBL172689 — IC50 = 60.0 nM 7.22
CHEMBL172286 — IC50 = 70.0 nM 7.16
CHEMBL172232 — IC50 = 70.0 nM 7.16
CHEMBL355790 — IC50 = 90.0 nM 7.05
CHEMBL368200 — IC50 = 100.0 nM 7.00
CHEMBL355529 — IC50 = 100.0 nM 7.00
CHEMBL173857 — IC50 = 140.0 nM 6.85
CHEMBL355528 — IC50 = 140.0 nM 6.85
CHEMBL368345 — IC50 = 140.0 nM 6.85
CHEMBL353440 — IC50 = 200.0 nM 6.70
CHEMBL170830 — IC50 = 200.0 nM 6.70
CHEMBL427114 — IC50 = 200.0 nM 6.70
CHEMBL172882 — IC50 = 260.0 nM 6.58
CHEMBL368455 — IC50 = 260.0 nM 6.58
CHEMBL174257 — IC50 = 270.0 nM 6.57
CHEMBL366533 — IC50 = 290.0 nM 6.54
CHEMBL368397 — IC50 = 370.0 nM 6.43
CHEMBL435669 — IC50 = 380.0 nM 6.42
CHEMBL170535 — IC50 = 390.0 nM 6.41
CHEMBL173908 — IC50 = 500.0 nM 6.30
CHEMBL366605 — IC50 = 540.0 nM 6.27
CHEMBL368543 — IC50 = 680.0 nM 6.17
CHEMBL367111 — IC50 = 680.0 nM 6.17
CHEMBL171242 — IC50 = 690.0 nM 6.16
CHEMBL354901 — IC50 = 730.0 nM 6.14
CHEMBL369668 — IC50 = 800.0 nM 6.10
CHEMBL369404 — IC50 = 1250.0 nM 5.90
CHEMBL366639 — IC50 = 1500.0 nM 5.82
CHEMBL174461 — IC50 = 1800.0 nM 5.75
CHEMBL367872 — IC50 = 2500.0 nM 5.60
CHEMBL367957 — IC50 = 4000.0 nM 5.40
CHEMBL170947 — IC50 = 6200.0 nM 5.21
CHEMBL366976 — IC50 = 8000.0 nM 5.10
CHEMBL367242 — IC50 = 12500.0 nM 4.90
CHEMBL354380 — IC50 = 14400.0 nM 4.84
CHEMBL368653 — IC50 = 15800.0 nM 4.80
CHEMBL173787 — IC50 > 1000.0 nM -
CHEMBL170836 — IC50 > 1000.0 nM -
CHEMBL174122 — IC50 > 1000.0 nM -
CHEMBL368350 — IC50 > 1000.0 nM -
CHEMBL353254 — IC50 > 32000.0 nM -
CHEMBL171392 — IC50 > 1000.0 nM -