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Assay Detail

CHEMBL3363471

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

Binding
Inhibition of p38alpha MAPK (unknown origin) by radiometric assay
27
Total Activities
27
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

Synthesis and structure-activity relationships of 4-fluorophenyl-imidazole p38α MAPK, CK1δ and JAK2 kinase inhibitors.
Seerden JP, Leusink-Ionescu G, Woudenberg-Vrenken T, Dros B, Molema G, Kamps JA, Kellogg RM.
Bioorg Med Chem Lett (2014) 24 : 3412 -3418
PubMed 24930833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.02 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3120970 1 8.07
CHEMBL278041 SB-202190 1 8.05
CHEMBL3314285 1 7.02
CHEMBL3120986 1 7.02
CHEMBL3314271 1 6.92
CHEMBL3120995 1 6.78
CHEMBL3120983 1 6.73
CHEMBL3120960 1 6.68
CHEMBL3314273 1 6.60
CHEMBL3120985 1 6.46
CHEMBL3120963 1 6.11
CHEMBL3314270 1 5.99
CHEMBL3314283 1 5.94
CHEMBL3120969 1 5.61
CHEMBL3314272 1 5.60
CHEMBL3314284 1 5.60
CHEMBL3313935 1 5.53
CHEMBL3314281 1 5.30
CHEMBL3314282 1 5.17
CHEMBL3314276 1 5.03
CHEMBL3314274 1 4.92
CHEMBL3314277 1 4.73
CHEMBL3314278 1 4.48
CHEMBL3314286 1 4.09
CHEMBL3314280 1 -
CHEMBL3314279 1 -
CHEMBL3314275 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3120970 IC50 = 8.5 nM 8.07
CHEMBL278041 SB-202190 IC50 = 9.0 nM 8.05
CHEMBL3314285 IC50 = 95.5 nM 7.02
CHEMBL3120986 IC50 = 96.0 nM 7.02
CHEMBL3314271 IC50 = 120.0 nM 6.92
CHEMBL3120995 IC50 = 166.0 nM 6.78
CHEMBL3120983 IC50 = 185.0 nM 6.73
CHEMBL3120960 IC50 = 210.0 nM 6.68
CHEMBL3314273 IC50 = 250.0 nM 6.60
CHEMBL3120985 IC50 = 345.0 nM 6.46
CHEMBL3120963 IC50 = 783.0 nM 6.11
CHEMBL3314270 IC50 = 1020.0 nM 5.99
CHEMBL3314283 IC50 = 1140.0 nM 5.94
CHEMBL3120969 IC50 = 2480.0 nM 5.61
CHEMBL3314272 IC50 = 2510.0 nM 5.60
CHEMBL3314284 IC50 = 2530.0 nM 5.60
CHEMBL3313935 IC50 = 2940.0 nM 5.53
CHEMBL3314281 IC50 = 4960.0 nM 5.30
CHEMBL3314282 IC50 = 6810.0 nM 5.17
CHEMBL3314276 IC50 = 9390.0 nM 5.03
CHEMBL3314274 IC50 = 12000.0 nM 4.92
CHEMBL3314277 IC50 = 18600.0 nM 4.73
CHEMBL3314278 IC50 = 32900.0 nM 4.48
CHEMBL3314286 IC50 = 82100.0 nM 4.09
CHEMBL3314280 IC50 > 100000.0 nM -
CHEMBL3314279 IC50 > 100000.0 nM -
CHEMBL3314275 IC50 > 100000.0 nM -