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Assay Detail

CHEMBL5320433

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

Binding
Inhibition of His-tagged human recombinant JNK1 expressed in insect cells incubated for 1 hr in presence of ATP by Z'-Lyte assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Insect cell
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 8 (CHEMBL2276)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of a Covalent Inhibitor of c-Jun N-Terminal Protein Kinase (JNK) 2/3 with Selectivity over JNK1.
Lu W, Liu Y, Gao Y, Geng Q, Gurbani D, Li L, Ficarro SB, Meyer CJ, Sinha D, You I, Tse J, He Z, Ji W, Che J, Kim AY, Yu T, Wen K, Anderson KC, Marto JA, Westover KD, Zhang T, Gray NS.
J Med Chem (2023) 66 : 3356 -3371
PubMed 36826833 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.90 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3393608 1 8.89
CHEMBL2216824 1 8.33
CHEMBL5432340 1 8.00
CHEMBL5415466 1 7.75
CHEMBL5397194 1 7.28
CHEMBL5436341 1 7.21
CHEMBL5396061 1 7.17
CHEMBL5436350 1 7.13
CHEMBL5410683 1 7.05
CHEMBL5398275 1 6.80
CHEMBL5413843 1 6.78
CHEMBL5395598 1 6.62
CHEMBL5433713 1 6.59
CHEMBL5408895 1 6.41
CHEMBL5406036 1 6.33
CHEMBL5437715 1 6.32
CHEMBL5410247 1 6.14
CHEMBL5415188 1 5.94
CHEMBL5398852 1 5.66
CHEMBL5406812 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3393608 IC50 = 1.3 nM 8.89
CHEMBL2216824 IC50 = 4.7 nM 8.33
CHEMBL5432340 IC50 = 10.0 nM 8.00
CHEMBL5415466 IC50 = 18.0 nM 7.75
CHEMBL5397194 IC50 = 53.0 nM 7.28
CHEMBL5436341 IC50 = 62.0 nM 7.21
CHEMBL5396061 IC50 = 67.0 nM 7.17
CHEMBL5436350 IC50 = 74.0 nM 7.13
CHEMBL5410683 IC50 = 89.0 nM 7.05
CHEMBL5398275 IC50 = 160.0 nM 6.80
CHEMBL5413843 IC50 = 166.0 nM 6.78
CHEMBL5395598 IC50 = 237.0 nM 6.62
CHEMBL5433713 IC50 = 256.0 nM 6.59
CHEMBL5408895 IC50 = 387.0 nM 6.41
CHEMBL5406036 IC50 = 470.0 nM 6.33
CHEMBL5437715 IC50 = 475.0 nM 6.32
CHEMBL5410247 IC50 = 724.0 nM 6.14
CHEMBL5415188 IC50 = 1140.0 nM 5.94
CHEMBL5398852 IC50 = 2173.0 nM 5.66
CHEMBL5406812 IC50 = 3047.0 nM 5.52