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Assay Detail

CHEMBL1107753

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

Binding
Inhibition of GST-tagged JAK2 kinase
44
Total Activities
44
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Tyrosine-protein kinase JAK2 (CHEMBL2971)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs).
Burns CJ, Bourke DG, Andrau L, Bu X, Charman SA, Donohue AC, Fantino E, Farrugia M, Feutrill JT, Joffe M, Kling MR, Kurek M, Nero TL, Nguyen T, Palmer JT, Phillips I, Shackleford DM, Sikanyika H, Styles M, Su S, Treutlein H, Zeng J, Wilks AF.
Bioorg Med Chem Lett (2009) 19 : 5887 -5892
PubMed 19762238 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 7.31 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1078889 1 8.70
CHEMBL1078274 1 8.52
CHEMBL1079077 1 8.40
CHEMBL1079078 1 8.22
CHEMBL1078275 1 8.22
CHEMBL1078005 1 8.10
CHEMBL1078277 1 8.10
CHEMBL1078689 1 8.05
CHEMBL1078166 1 8.00
CHEMBL1078276 1 7.96
CHEMBL1078688 1 7.92
CHEMBL1078866 1 7.85
CHEMBL1080411 1 7.80
CHEMBL1078767 1 7.80
CHEMBL1078178 MOMELOTINIB 4.0 1 7.75
CHEMBL1078971 1 7.75
CHEMBL1078364 1 7.52
CHEMBL221959 TOFACITINIB 4.0 1 7.48
CHEMBL1081138 1 7.48
CHEMBL1078934 1 7.39
CHEMBL1078933 1 7.33
CHEMBL1077842 1 7.28
CHEMBL1078363 1 7.19
CHEMBL1077458 1 7.17
CHEMBL1077841 1 7.16
CHEMBL1080955 1 7.09
CHEMBL1080954 1 7.08
CHEMBL1077431 1 7.06
CHEMBL1078229 1 6.95
CHEMBL1078228 1 6.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1078889 IC50 = 2.0 nM 8.70
CHEMBL1078274 IC50 = 3.0 nM 8.52
CHEMBL1079077 IC50 = 4.0 nM 8.40
CHEMBL1079078 IC50 = 6.0 nM 8.22
CHEMBL1078275 IC50 = 6.0 nM 8.22
CHEMBL1078005 IC50 = 8.0 nM 8.10
CHEMBL1078277 IC50 = 8.0 nM 8.10
CHEMBL1078689 IC50 = 9.0 nM 8.05
CHEMBL1078166 IC50 = 10.0 nM 8.00
CHEMBL1078276 IC50 = 11.0 nM 7.96
CHEMBL1078688 IC50 = 12.0 nM 7.92
CHEMBL1078866 IC50 = 14.0 nM 7.85
CHEMBL1080411 IC50 = 16.0 nM 7.80
CHEMBL1078767 IC50 = 16.0 nM 7.80
CHEMBL1078971 IC50 = 18.0 nM 7.75
CHEMBL1078178 MOMELOTINIB IC50 = 18.0 nM 7.75
CHEMBL1078364 IC50 = 30.0 nM 7.52
CHEMBL221959 TOFACITINIB IC50 = 33.0 nM 7.48
CHEMBL1081138 IC50 = 33.0 nM 7.48
CHEMBL1078934 IC50 = 41.0 nM 7.39
CHEMBL1078933 IC50 = 47.0 nM 7.33
CHEMBL1077842 IC50 = 52.0 nM 7.28
CHEMBL1078363 IC50 = 65.0 nM 7.19
CHEMBL1077458 IC50 = 67.0 nM 7.17
CHEMBL1077841 IC50 = 69.0 nM 7.16
CHEMBL1080955 IC50 = 81.0 nM 7.09
CHEMBL1080954 IC50 = 83.0 nM 7.08
CHEMBL1077431 IC50 = 88.0 nM 7.06
CHEMBL1078229 IC50 = 113.0 nM 6.95
CHEMBL1078228 IC50 = 116.0 nM 6.94
CHEMBL1078165 IC50 = 132.0 nM 6.88
CHEMBL1078721 IC50 = 163.0 nM 6.79
CHEMBL1078720 IC50 = 166.0 nM 6.78
CHEMBL1079120 IC50 = 186.0 nM 6.73
CHEMBL1079690 IC50 = 202.0 nM 6.70
CHEMBL1078370 IC50 = 298.0 nM 6.53
CHEMBL1077575 IC50 = 303.0 nM 6.52
CHEMBL1080395 IC50 = 326.0 nM 6.49
CHEMBL1079689 IC50 = 322.0 nM 6.49
CHEMBL1079121 IC50 = 374.0 nM 6.43
CHEMBL1080394 IC50 = 467.0 nM 6.33
CHEMBL1078984 IC50 = 533.0 nM 6.27
CHEMBL1078453 IC50 = 549.0 nM 6.26
CHEMBL1078159 IC50 = 545.0 nM 6.26