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Assay Detail

CHEMBL4842274

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

Binding
Inhibition of JNK2 (unknown origin) assessed as reduction in phosphorylated ULight-labeled 4EBP1 peptide measured after 1 hr by time-resolved fluorescence assay
16
Total Activities
16
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 9 (CHEMBL4179)
Type SINGLE PROTEIN
Organism Homo sapiens

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 16 7.64 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1950289 TANZISERTIB 2.0 1 8.30
CHEMBL4878046 1 8.30
CHEMBL4847078 1 8.30
CHEMBL4877560 1 8.30
CHEMBL4853125 1 8.22
CHEMBL4862452 1 7.89
CHEMBL4874549 1 7.75
CHEMBL4872066 1 7.68
CHEMBL4861369 1 7.58
CHEMBL4847106 CC-90001 2.0 1 7.51
CHEMBL4852708 1 7.51
CHEMBL4874419 1 7.10
CHEMBL4852680 1 6.96
CHEMBL4848290 1 6.95
CHEMBL4848796 1 6.94
CHEMBL4877655 1 6.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1950289 TANZISERTIB IC50 = 5.0 nM 8.30
CHEMBL4878046 IC50 = 5.0 nM 8.30
CHEMBL4847078 IC50 = 5.0 nM 8.30
CHEMBL4877560 IC50 = 5.0 nM 8.30
CHEMBL4853125 IC50 = 6.0 nM 8.22
CHEMBL4862452 IC50 = 13.0 nM 7.89
CHEMBL4874549 IC50 = 18.0 nM 7.75
CHEMBL4872066 IC50 = 21.0 nM 7.68
CHEMBL4861369 IC50 = 26.0 nM 7.58
CHEMBL4847106 CC-90001 IC50 = 31.0 nM 7.51
CHEMBL4852708 IC50 = 31.0 nM 7.51
CHEMBL4874419 IC50 = 79.0 nM 7.10
CHEMBL4852680 IC50 = 110.0 nM 6.96
CHEMBL4848290 IC50 = 113.0 nM 6.95
CHEMBL4848796 IC50 = 114.0 nM 6.94
CHEMBL4877655 IC50 = 120.0 nM 6.92