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Assay Detail

CHEMBL4842271

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

Binding
Inhibition of JNK1 in mouse RAW264.7 cells assessed as inhibition of c-Jun phosphorylation incubated for 30 mins by cellular assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type RAW264.7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 8 (CHEMBL1795174)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of the c-Jun N-Terminal Kinase Inhibitor <b>CC-90001</b>.
Nagy MA, Hilgraf R, Mortensen DS, Elsner J, Norris S, Tikhe J, Yoon W, Paisner D, Delgado M, Erdman P, Haelewyn J, Khambatta G, Xu L, Romanow WJ, Condroski K, Bahmanyar S, McCarrick M, Benish B, Blease K, LeBrun L, Moghaddam MF, Apuy J, Canan SS, Bennett BL, Satoh Y.
J Med Chem (2021) 64 : 18193 -18208
PubMed 34894681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.06 6.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4862452 1 6.77
CHEMBL4877655 1 6.68
CHEMBL4878046 1 6.67
CHEMBL4874549 1 6.46
CHEMBL4847078 1 6.40
CHEMBL4872066 1 6.26
CHEMBL4853125 1 6.24
CHEMBL1950289 TANZISERTIB 2.0 1 5.95
CHEMBL4861369 1 5.84
CHEMBL4874419 1 5.75
CHEMBL4848290 1 5.62
CHEMBL4848796 1 5.17
CHEMBL4852680 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4862452 IC50 = 170.0 nM 6.77
CHEMBL4877655 IC50 = 210.0 nM 6.68
CHEMBL4878046 IC50 = 212.0 nM 6.67
CHEMBL4874549 IC50 = 350.0 nM 6.46
CHEMBL4847078 IC50 = 400.0 nM 6.40
CHEMBL4872066 IC50 = 550.0 nM 6.26
CHEMBL4853125 IC50 = 580.0 nM 6.24
CHEMBL1950289 TANZISERTIB IC50 = 1120.0 nM 5.95
CHEMBL4861369 IC50 = 1450.0 nM 5.84
CHEMBL4874419 IC50 = 1770.0 nM 5.75
CHEMBL4848290 IC50 = 2390.0 nM 5.62
CHEMBL4848796 IC50 = 6800.0 nM 5.17
CHEMBL4852680 IC50 = 10100.0 nM 5.00