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Assay Detail

CHEMBL860185

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

Functional
Inhibition of cJun phosphorylation in HepG2 cell line
23
Total Activities
18
Compounds Tested
2
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

Aminopyridine-based c-Jun N-terminal kinase inhibitors with cellular activity and minimal cross-kinase activity.
Szczepankiewicz BG, Kosogof C, Nelson LT, Liu G, Liu B, Zhao H, Serby MD, Xin Z, Liu M, Gum RJ, Haasch DL, Wang S, Clampit JE, Johnson EF, Lubben TH, Stashko MA, Olejniczak ET, Sun C, Dorwin SA, Haskins K, Abad-Zapatero C, Fry EH, Hutchins CW, Sham HL, Rondinone CM, Trevillyan JM.
J Med Chem (2006) 49 : 3563 -3580
PubMed 16759099 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 5.80 6.55
Ki 6 7.47 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378627 2 8.40
CHEMBL210618 2 8.40
CHEMBL210963 2 8.05
CHEMBL210928 2 7.89
CHEMBL209769 1 6.55
CHEMBL208637 2 6.36
CHEMBL382639 1 6.05
CHEMBL209505 1 6.04
CHEMBL426134 1 5.85
CHEMBL211009 1 5.85
CHEMBL210655 1 5.85
CHEMBL210462 1 5.80
CHEMBL210032 1 5.72
CHEMBL209291 1 5.60
CHEMBL209192 1 5.47
CHEMBL377578 1 5.41
CHEMBL383308 1 5.26
CHEMBL209669 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378627 Ki = 4.0 nM 8.40
CHEMBL210618 Ki = 4.0 nM 8.40
CHEMBL210963 Ki = 9.0 nM 8.05
CHEMBL210928 Ki = 13.0 nM 7.89
CHEMBL209769 EC50 = 280.0 nM 6.55
CHEMBL208637 Ki = 440.0 nM 6.36
CHEMBL378627 EC50 = 650.0 nM 6.19
CHEMBL382639 EC50 = 890.0 nM 6.05
CHEMBL209505 EC50 = 910.0 nM 6.04
CHEMBL210618 EC50 = 920.0 nM 6.04
CHEMBL210963 EC50 = 1300.0 nM 5.89
CHEMBL210655 EC50 = 1400.0 nM 5.85
CHEMBL426134 EC50 = 1400.0 nM 5.85
CHEMBL211009 EC50 = 1400.0 nM 5.85
CHEMBL210462 EC50 = 1600.0 nM 5.80
CHEMBL210928 EC50 = 1750.0 nM 5.76
CHEMBL210032 Ki = 1900.0 nM 5.72
CHEMBL209291 EC50 = 2500.0 nM 5.60
CHEMBL209192 EC50 = 3400.0 nM 5.47
CHEMBL377578 EC50 = 3900.0 nM 5.41
CHEMBL383308 EC50 = 5500.0 nM 5.26
CHEMBL208637 EC50 = 6800.0 nM 5.17
CHEMBL209669 EC50 > 10000.0 nM -