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Assay Detail

CHEMBL1825596

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

Binding
Inhibition of recombinant JNK3 using ser73 of c-jun as substrate preincubated for 15 mins measured after 60 mins by TR-FRET assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Mitogen-activated protein kinase 10 (CHEMBL2637)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of brain penetrant selective JNK inhibitors with improved pharmacokinetic properties for the prevention of neurodegeneration.
Bowers S, Truong AP, Jeffrey Neitz R, Hom RK, Sealy JM, Probst GD, Quincy D, Peterson B, Chan W, Galemmo RA, Konradi AW, Sham HL, Tóth G, Pan H, Lin M, Yao N, Artis DR, Zhang H, Chen L, Dryer M, Samant B, Zmolek W, Wong K, Lorentzen C, Goldbach E, Tonn G, Quinn KP, Sauer JM, Wright S, Powell K, Ruslim L, Ren Z, Bard F, Yednock TA, Griswold-Prenner I.
Bioorg Med Chem Lett (2011) 21 : 5521 -5527
PubMed 21813278 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.88 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1822151 1 8.70
CHEMBL1822152 1 8.70
CHEMBL1822305 1 8.52
CHEMBL1822145 1 8.30
CHEMBL1822153 1 8.22
CHEMBL1822149 1 8.22
CHEMBL1822139 1 8.22
CHEMBL1822141 1 8.22
CHEMBL1822140 1 8.15
CHEMBL1822309 1 8.10
CHEMBL1822307 1 8.10
CHEMBL1822143 1 8.10
CHEMBL1822308 1 8.05
CHEMBL1822147 1 8.05
CHEMBL1822146 1 8.05
CHEMBL1822306 1 7.96
CHEMBL1822144 1 7.85
CHEMBL1822138 1 7.85
CHEMBL1822142 1 7.85
CHEMBL1822154 1 7.82
CHEMBL1822150 1 7.72
CHEMBL1822132 1 7.62
CHEMBL1682013 1 7.55
CHEMBL1822133 1 7.52
CHEMBL1822134 1 7.39
CHEMBL1822135 1 7.28
CHEMBL1822148 1 7.15
CHEMBL1822137 1 6.74
CHEMBL1822136 1 6.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1822151 IC50 = 2.0 nM 8.70
CHEMBL1822152 IC50 = 2.0 nM 8.70
CHEMBL1822305 IC50 = 3.0 nM 8.52
CHEMBL1822145 IC50 = 5.0 nM 8.30
CHEMBL1822153 IC50 = 6.0 nM 8.22
CHEMBL1822149 IC50 = 6.0 nM 8.22
CHEMBL1822139 IC50 = 6.0 nM 8.22
CHEMBL1822141 IC50 = 6.0 nM 8.22
CHEMBL1822140 IC50 = 7.0 nM 8.15
CHEMBL1822309 IC50 = 8.0 nM 8.10
CHEMBL1822307 IC50 = 8.0 nM 8.10
CHEMBL1822143 IC50 = 8.0 nM 8.10
CHEMBL1822308 IC50 = 9.0 nM 8.05
CHEMBL1822147 IC50 = 9.0 nM 8.05
CHEMBL1822146 IC50 = 9.0 nM 8.05
CHEMBL1822306 IC50 = 11.0 nM 7.96
CHEMBL1822144 IC50 = 14.0 nM 7.85
CHEMBL1822138 IC50 = 14.0 nM 7.85
CHEMBL1822142 IC50 = 14.0 nM 7.85
CHEMBL1822154 IC50 = 15.0 nM 7.82
CHEMBL1822150 IC50 = 19.0 nM 7.72
CHEMBL1822132 IC50 = 24.0 nM 7.62
CHEMBL1682013 IC50 = 28.0 nM 7.55
CHEMBL1822133 IC50 = 30.0 nM 7.52
CHEMBL1822134 IC50 = 41.0 nM 7.39
CHEMBL1822135 IC50 = 52.0 nM 7.28
CHEMBL1822148 IC50 = 71.0 nM 7.15
CHEMBL1822137 IC50 = 183.0 nM 6.74
CHEMBL1822136 IC50 = 280.0 nM 6.55