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Assay Detail

CHEMBL1952892

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

Binding
Inhibition of hexa-His-tagged JNK2 expressed in baculoviral system using GST-tagged cJun as substrate preincubated for 15 mins prior ATP addition measured after 60 mins by scintillation counting
4
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase 9 (CHEMBL4179)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of CC-930, an orally active anti-fibrotic JNK inhibitor.
Plantevin Krenitsky V, Nadolny L, Delgado M, Ayala L, Clareen SS, Hilgraf R, Albers R, Hegde S, D'Sidocky N, Sapienza J, Wright J, McCarrick M, Bahmanyar S, Chamberlain P, Delker SL, Muir J, Giegel D, Xu L, Celeridad M, Lachowitzer J, Bennett B, Moghaddam M, Khatsenko O, Katz J, Fan R, Bai A, Tang Y, Shirley MA, Benish B, Bodine T, Blease K, Raymon H, Cathers BE, Satoh Y.
Bioorg Med Chem Lett (2012) 22 : 1433 -1438
PubMed 22244937 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.86 8.15
Ki 1 8.21 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1950289 TANZISERTIB 2.0 2 8.21
CHEMBL1950304 1 8.00
CHEMBL1950303 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1950289 TANZISERTIB Ki = 6.2 nM 8.21
CHEMBL1950289 TANZISERTIB IC50 = 7.0 nM 8.15
CHEMBL1950304 IC50 = 10.0 nM 8.00
CHEMBL1950303 IC50 = 38.0 nM 7.42