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Assay Detail

CHEMBL866024

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Functional
Inhibition of cJun phosphorylation in HepG2 cells
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HepG2
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

c-Jun N-terminal kinase, JNK (CHEMBL2096667)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Discovery of potent, highly selective, and orally bioavailable pyridine carboxamide c-Jun NH2-terminal kinase inhibitors.
Zhao H, Serby MD, Xin Z, Szczepankiewicz BG, Liu M, Kosogof C, Liu B, Nelson LT, Johnson EF, Wang S, Pederson T, Gum RJ, Clampit JE, Haasch DL, Abad-Zapatero C, Fry EH, Rondinone C, Trevillyan JM, Sham HL, Liu G.
J Med Chem (2006) 49 : 4455 -4458
PubMed 16854050 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.10 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL377408 1 6.96
CHEMBL439323 1 6.39
CHEMBL377383 1 6.32
CHEMBL424872 1 6.28
CHEMBL214212 1 6.19
CHEMBL211195 1 5.96
CHEMBL209534 1 5.92
CHEMBL209740 1 5.60
CHEMBL377991 1 5.24
CHEMBL209397 1 -
CHEMBL378955 1 -
CHEMBL211584 1 -
CHEMBL211605 1 -
CHEMBL209049 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL377408 IC50 = 110.0 nM 6.96
CHEMBL439323 IC50 = 410.0 nM 6.39
CHEMBL377383 IC50 = 480.0 nM 6.32
CHEMBL424872 IC50 = 530.0 nM 6.28
CHEMBL214212 IC50 = 640.0 nM 6.19
CHEMBL211195 IC50 = 1100.0 nM 5.96
CHEMBL209534 IC50 = 1200.0 nM 5.92
CHEMBL209740 IC50 = 2500.0 nM 5.60
CHEMBL377991 IC50 = 5800.0 nM 5.24
CHEMBL209397 IC50 - -
CHEMBL378955 IC50 > 10000.0 nM -
CHEMBL211584 IC50 > 10000.0 nM -
CHEMBL211605 IC50 - -
CHEMBL209049 IC50 - -