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Assay Detail

CHEMBL987298

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

Binding
Displacement of rhodamine-green labeled (2-(6-amino-3-imino-3H-xanthen-9-yl)-5-{[({4-[4-(4-Cl-3-hydroxyphenyl)-5-(4-pyridinyl)-1H-imidazol-2yl]phenyl}methyl)amino]carbonyl}benzoic acid from human p38alpha by fluorescence polarization
26
Total Activities
26
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

Biphenyl amide p38 kinase inhibitors 4: DFG-in and DFG-out binding modes.
Angell RM, Angell TD, Bamborough P, Bamford MJ, Chung CW, Cockerill SG, Flack SS, Jones KL, Laine DI, Longstaff T, Ludbrook S, Pearson R, Smith KJ, Smee PA, Somers DO, Walker AL.
Bioorg Med Chem Lett (2008) 18 : 4433 -4437
PubMed 18602262 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 7.87 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL477190 1 9.22
CHEMBL476996 1 8.80
CHEMBL477182 GW769076X 1 8.72
CHEMBL515466 1 8.72
CHEMBL476995 1 8.68
CHEMBL476141 1 8.60
CHEMBL477191 1 8.52
CHEMBL476351 GW775608X 1 8.36
CHEMBL478234 1 8.34
CHEMBL478656 1 8.28
CHEMBL478031 1 8.20
CHEMBL103667 DORAMAPIMOD 2.0 1 8.19
CHEMBL514509 1 7.96
CHEMBL478649 1 7.92
CHEMBL478421 1 7.92
CHEMBL515318 1 7.85
CHEMBL477583 GW743024X 1 7.82
CHEMBL514207 1 7.82
CHEMBL95692 SB-242235 1 7.44
CHEMBL516264 1 7.14
CHEMBL476752 1 7.10
CHEMBL477620 1 7.00
CHEMBL478225 1 6.82
CHEMBL270164 GW607117X 1 6.62
CHEMBL476552 1 6.52
CHEMBL476111 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL477190 Ki = 0.6 nM 9.22
CHEMBL476996 Ki = 1.6 nM 8.80
CHEMBL477182 GW769076X Ki = 1.9 nM 8.72
CHEMBL515466 Ki = 1.9 nM 8.72
CHEMBL476995 Ki = 2.1 nM 8.68
CHEMBL476141 Ki = 2.5 nM 8.60
CHEMBL477191 Ki = 3.0 nM 8.52
CHEMBL476351 GW775608X Ki = 4.4 nM 8.36
CHEMBL478234 Ki = 4.6 nM 8.34
CHEMBL478656 Ki = 5.2 nM 8.28
CHEMBL478031 Ki = 6.3 nM 8.20
CHEMBL103667 DORAMAPIMOD Ki = 6.4 nM 8.19
CHEMBL514509 Ki = 11.0 nM 7.96
CHEMBL478649 Ki = 12.0 nM 7.92
CHEMBL478421 Ki = 12.0 nM 7.92
CHEMBL515318 Ki = 14.0 nM 7.85
CHEMBL477583 GW743024X Ki = 15.0 nM 7.82
CHEMBL514207 Ki = 15.0 nM 7.82
CHEMBL95692 SB-242235 Ki = 36.0 nM 7.44
CHEMBL516264 Ki = 73.0 nM 7.14
CHEMBL476752 Ki = 79.0 nM 7.10
CHEMBL477620 Ki = 100.0 nM 7.00
CHEMBL478225 Ki = 150.0 nM 6.82
CHEMBL270164 GW607117X Ki = 240.0 nM 6.62
CHEMBL476552 Ki = 300.0 nM 6.52
CHEMBL476111 Ki = 730.0 nM 6.14