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Assay Detail

CHEMBL1042604

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Binding
Inhibition of c-jun phosphorylation in rat INS-1 cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type INS1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis, biological evaluation, X-ray structure, and pharmacokinetics of aminopyrimidine c-jun-N-terminal kinase (JNK) inhibitors.
Kamenecka T, Jiang R, Song X, Duckett D, Chen W, Ling YY, Habel J, Laughlin JD, Chambers J, Figuera-Losada M, Cameron MD, Lin L, Ruiz CH, LoGrasso PV.
J Med Chem (2010) 53 : 419 -431
PubMed 19947601 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.85 7.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL585951 1 7.27
CHEMBL584899 1 7.09
CHEMBL571023 1 7.08
CHEMBL570554 1 7.05
CHEMBL571434 1 6.85
CHEMBL571626 1 6.68
CHEMBL568116 1 6.58
CHEMBL585725 1 6.55
CHEMBL572283 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL585951 IC50 = 54.0 nM 7.27
CHEMBL584899 IC50 = 82.0 nM 7.09
CHEMBL571023 IC50 = 83.0 nM 7.08
CHEMBL570554 IC50 = 89.0 nM 7.05
CHEMBL571434 IC50 = 140.0 nM 6.85
CHEMBL571626 IC50 = 210.0 nM 6.68
CHEMBL568116 IC50 = 260.0 nM 6.58
CHEMBL585725 IC50 = 281.0 nM 6.55
CHEMBL572283 IC50 = 350.0 nM 6.46