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Assay Detail

CHEMBL860181

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

Binding
Inhibition of JNK1-mediated ATF2 phosphorylation
ChEMBL ↗
62
Total Activities
56
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mitogen-activated protein kinase 8 (CHEMBL2276) ↗
Type SINGLE PROTEIN
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
IC50 56 6.33 7.85
Ki 6 7.95 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL378627 — — 2 9.00
CHEMBL210618 — — 2 8.70
CHEMBL210928 — — 2 8.52
CHEMBL210963 — — 2 8.52
CHEMBL209769 — — 1 7.46
CHEMBL209669 — — 1 7.16
CHEMBL209505 — — 1 7.16
CHEMBL210462 — — 1 7.13
CHEMBL382639 — — 1 7.11
CHEMBL377578 — — 1 7.06
CHEMBL211009 — — 1 6.96
CHEMBL210655 — — 1 6.92
CHEMBL383308 — — 1 6.80
CHEMBL426134 — — 1 6.75
CHEMBL208637 — — 2 6.72
CHEMBL209192 — — 1 6.72
CHEMBL209291 — — 1 6.68
CHEMBL208877 — — 1 6.57
CHEMBL210586 — — 1 6.52
CHEMBL209770 — — 1 6.52
CHEMBL378931 — — 1 6.51
CHEMBL378499 — — 1 6.46
CHEMBL380152 — — 1 6.40
CHEMBL208558 — — 1 6.40
CHEMBL208447 — — 1 6.38
CHEMBL425413 — — 1 6.29
CHEMBL210032 — — 2 6.26
CHEMBL210861 — — 1 6.24
CHEMBL209292 — — 1 6.24
CHEMBL210256 — — 1 6.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL378627 — Ki = 1.0 nM 9.00
CHEMBL210618 — Ki = 2.0 nM 8.70
CHEMBL210963 — Ki = 3.0 nM 8.52
CHEMBL210928 — Ki = 3.0 nM 8.52
CHEMBL378627 — IC50 = 14.0 nM 7.85
CHEMBL209769 — IC50 = 35.0 nM 7.46
CHEMBL210928 — IC50 = 36.0 nM 7.44
CHEMBL210963 — IC50 = 38.0 nM 7.42
CHEMBL210618 — IC50 = 45.0 nM 7.35
CHEMBL209505 — IC50 = 69.0 nM 7.16
CHEMBL209669 — IC50 = 69.0 nM 7.16
CHEMBL210462 — IC50 = 74.0 nM 7.13
CHEMBL382639 — IC50 = 77.0 nM 7.11
CHEMBL377578 — IC50 = 87.0 nM 7.06
CHEMBL211009 — IC50 = 110.0 nM 6.96
CHEMBL210655 — IC50 = 120.0 nM 6.92
CHEMBL383308 — IC50 = 160.0 nM 6.80
CHEMBL426134 — IC50 = 180.0 nM 6.75
CHEMBL208637 — Ki = 190.0 nM 6.72
CHEMBL209192 — IC50 = 190.0 nM 6.72
CHEMBL209291 — IC50 = 210.0 nM 6.68
CHEMBL208877 — IC50 = 270.0 nM 6.57
CHEMBL209770 — IC50 = 300.0 nM 6.52
CHEMBL210586 — IC50 = 300.0 nM 6.52
CHEMBL378931 — IC50 = 310.0 nM 6.51
CHEMBL378499 — IC50 = 350.0 nM 6.46
CHEMBL380152 — IC50 = 400.0 nM 6.40
CHEMBL208558 — IC50 = 400.0 nM 6.40
CHEMBL208447 — IC50 = 420.0 nM 6.38
CHEMBL425413 — IC50 = 510.0 nM 6.29
CHEMBL210032 — Ki = 550.0 nM 6.26
CHEMBL209292 — IC50 = 580.0 nM 6.24
CHEMBL210861 — IC50 = 570.0 nM 6.24
CHEMBL210256 — IC50 = 750.0 nM 6.12
CHEMBL208637 — IC50 = 750.0 nM 6.12
CHEMBL377348 — IC50 = 890.0 nM 6.05
CHEMBL209136 — IC50 = 910.0 nM 6.04
CHEMBL377201 — IC50 = 1100.0 nM 5.96
CHEMBL210222 — IC50 = 1400.0 nM 5.85
CHEMBL380279 — IC50 = 1700.0 nM 5.77
CHEMBL210032 — IC50 = 1900.0 nM 5.72
CHEMBL378980 — IC50 = 2100.0 nM 5.68
CHEMBL210363 — IC50 = 2200.0 nM 5.66
CHEMBL380044 — IC50 = 2400.0 nM 5.62
CHEMBL210737 — IC50 = 2600.0 nM 5.58
CHEMBL209299 — IC50 = 2700.0 nM 5.57
CHEMBL379414 — IC50 = 3000.0 nM 5.52
CHEMBL210752 — IC50 = 3500.0 nM 5.46
CHEMBL209082 — IC50 = 4000.0 nM 5.40
CHEMBL208448 — IC50 = 4400.0 nM 5.36