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Assay Detail

CHEMBL733336

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Binding
Kd value and murine Mitogen-activated protein kinase p38 alpha complex was calculated
27
Total Activities
27
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 (CHEMBL2336)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Structure-activity relationships of the p38alpha MAP kinase inhibitor 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)naph- thalen-1-yl]urea (BIRB 796).
Regan J, Capolino A, Cirillo PF, Gilmore T, Graham AG, Hickey E, Kroe RR, Madwed J, Moriak M, Nelson R, Pargellis CA, Swinamer A, Torcellini C, Tsang M, Moss N.
J Med Chem (2003) 46 : 4676 -4686
PubMed 14561087 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 27 8.58 10.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103667 DORAMAPIMOD 2.0 1 10.34
CHEMBL336001 1 10.13
CHEMBL143886 1 10.02
CHEMBL143134 1 10.00
CHEMBL344625 1 9.80
CHEMBL104991 1 9.74
CHEMBL344800 1 9.64
CHEMBL318810 1 9.64
CHEMBL142115 1 9.40
CHEMBL343227 1 9.28
CHEMBL143373 1 9.06
CHEMBL139991 1 8.82
CHEMBL348228 1 8.72
CHEMBL105248 1 8.47
CHEMBL143141 1 8.46
CHEMBL143207 1 8.23
CHEMBL342523 1 8.00
CHEMBL342952 1 7.96
CHEMBL336681 1 7.92
CHEMBL424107 1 7.85
CHEMBL10 SB-203580 1 7.70
CHEMBL423196 1 7.64
CHEMBL104749 1 7.58
CHEMBL107850 1 7.25
CHEMBL141294 1 7.19
CHEMBL341559 1 7.19
CHEMBL104119 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103667 DORAMAPIMOD Kd = 0.046 nM 10.34
CHEMBL336001 Kd = 0.074 nM 10.13
CHEMBL143886 Kd = 0.096 nM 10.02
CHEMBL143134 Kd = 0.1 nM 10.00
CHEMBL344625 Kd = 0.16 nM 9.80
CHEMBL104991 Kd = 0.18 nM 9.74
CHEMBL344800 Kd = 0.23 nM 9.64
CHEMBL318810 Kd = 0.23 nM 9.64
CHEMBL142115 Kd = 0.4 nM 9.40
CHEMBL343227 Kd = 0.52 nM 9.28
CHEMBL143373 Kd = 0.87 nM 9.06
CHEMBL139991 Kd = 1.5 nM 8.82
CHEMBL348228 Kd = 1.9 nM 8.72
CHEMBL105248 Kd = 3.4 nM 8.47
CHEMBL143141 Kd = 3.5 nM 8.46
CHEMBL143207 Kd = 5.9 nM 8.23
CHEMBL342523 Kd = 9.9 nM 8.00
CHEMBL342952 Kd = 11.0 nM 7.96
CHEMBL336681 Kd = 12.0 nM 7.92
CHEMBL424107 Kd = 14.0 nM 7.85
CHEMBL10 SB-203580 Kd = 20.0 nM 7.70
CHEMBL423196 Kd = 23.0 nM 7.64
CHEMBL104749 Kd = 26.0 nM 7.58
CHEMBL107850 Kd = 56.0 nM 7.25
CHEMBL141294 Kd = 64.0 nM 7.19
CHEMBL341559 Kd = 64.0 nM 7.19
CHEMBL104119 Kd = 2400.0 nM 5.62