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Assay Detail

CHEMBL732624

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

Binding
In vitro inhibitory concentration against Mitogen-activated protein kinase p38 alpha
22
Total Activities
22
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

Design and synthesis of 4-azaindoles as inhibitors of p38 MAP kinase.
Trejo A, Arzeno H, Browner M, Chanda S, Cheng S, Comer DD, Dalrymple SA, Dunten P, Lafargue J, Lovejoy B, Freire-Moar J, Lim J, Mcintosh J, Miller J, Papp E, Reuter D, Roberts R, Sanpablo F, Saunders J, Song K, Villasenor A, Warren SD, Welch M, Weller P, Whiteley PE, Zeng L, Goldstein DM.
J Med Chem (2003) 46 : 4702 -4713
PubMed 14561090 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.05 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL142425 1 9.00
CHEMBL358537 1 9.00
CHEMBL142367 1 8.52
CHEMBL143476 1 8.52
CHEMBL142753 1 8.30
CHEMBL344955 1 8.19
CHEMBL356756 1 7.68
CHEMBL342503 1 7.62
CHEMBL143307 1 7.28
CHEMBL358548 1 7.17
CHEMBL142523 1 7.07
CHEMBL336002 1 7.01
CHEMBL356355 1 6.76
CHEMBL141999 1 6.73
CHEMBL143389 1 6.66
CHEMBL313417 1 6.40
CHEMBL142381 1 6.05
CHEMBL345095 1 5.75
CHEMBL358718 1 5.71
CHEMBL343873 1 5.51
CHEMBL142682 1 5.48
CHEMBL343481 1 4.63

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL142425 IC50 = 1.0 nM 9.00
CHEMBL358537 IC50 = 1.0 nM 9.00
CHEMBL142367 IC50 = 3.0 nM 8.52
CHEMBL143476 IC50 = 3.0 nM 8.52
CHEMBL142753 IC50 = 5.0 nM 8.30
CHEMBL344955 IC50 = 6.5 nM 8.19
CHEMBL356756 IC50 = 21.0 nM 7.68
CHEMBL342503 IC50 = 24.0 nM 7.62
CHEMBL143307 IC50 = 53.0 nM 7.28
CHEMBL358548 IC50 = 68.0 nM 7.17
CHEMBL142523 IC50 = 86.0 nM 7.07
CHEMBL336002 IC50 = 98.0 nM 7.01
CHEMBL356355 IC50 = 172.0 nM 6.76
CHEMBL141999 IC50 = 185.0 nM 6.73
CHEMBL143389 IC50 = 217.0 nM 6.66
CHEMBL313417 IC50 = 400.0 nM 6.40
CHEMBL142381 IC50 = 895.0 nM 6.05
CHEMBL345095 IC50 = 1800.0 nM 5.75
CHEMBL358718 IC50 = 1970.0 nM 5.71
CHEMBL343873 IC50 = 3100.0 nM 5.51
CHEMBL142682 IC50 = 3300.0 nM 5.48
CHEMBL343481 IC50 = 23600.0 nM 4.63