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Assay Detail

CHEMBL2186596

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

Binding
Inhibition of purified JAK2 incubated for 30 mins
31
Total Activities
31
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

Discovery of potent and selective pyrazolopyrimidine janus kinase 2 inhibitors.
Hanan EJ, van Abbema A, Barrett K, Blair WS, Blaney J, Chang C, Eigenbrot C, Flynn S, Gibbons P, Hurley CA, Kenny JR, Kulagowski J, Lee L, Magnuson SR, Morris C, Murray J, Pastor RM, Rawson T, Siu M, Ultsch M, Zhou A, Sampath D, Lyssikatos JP.
J Med Chem (2012) 55 : 10090 -10107
PubMed 23061660 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 31 8.45 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2178804 1 10.00
CHEMBL2178805 1 10.00
CHEMBL1789941 RUXOLITINIB 4.0 1 9.62
CHEMBL2178803 1 9.52
CHEMBL2178801 1 9.52
CHEMBL2178799 1 9.40
CHEMBL2178800 1 9.22
CHEMBL2178258 1 9.00
CHEMBL2178254 1 9.00
CHEMBL2178255 1 8.89
CHEMBL2178802 1 8.80
CHEMBL2178257 1 8.74
CHEMBL2178266 1 8.68
CHEMBL2178807 1 8.60
CHEMBL2178253 1 8.49
CHEMBL2178252 1 8.49
CHEMBL2178247 1 8.29
CHEMBL2177122 1 8.28
CHEMBL2178260 1 8.25
CHEMBL2178249 1 8.15
CHEMBL2178250 1 8.01
CHEMBL2178806 1 7.92
CHEMBL2178261 1 7.85
CHEMBL2178248 1 7.81
CHEMBL2178263 1 7.78
CHEMBL2178256 1 7.50
CHEMBL2178262 1 7.39
CHEMBL2178264 1 7.38
CHEMBL2178259 1 7.31
CHEMBL2178265 1 7.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2178804 Ki = 0.1 nM 10.00
CHEMBL2178805 Ki = 0.1 nM 10.00
CHEMBL1789941 RUXOLITINIB Ki = 0.24 nM 9.62
CHEMBL2178803 Ki = 0.3 nM 9.52
CHEMBL2178801 Ki = 0.3 nM 9.52
CHEMBL2178799 Ki = 0.4 nM 9.40
CHEMBL2178800 Ki = 0.6 nM 9.22
CHEMBL2178258 Ki = 1.0 nM 9.00
CHEMBL2178254 Ki = 1.0 nM 9.00
CHEMBL2178255 Ki = 1.3 nM 8.89
CHEMBL2178802 Ki = 1.6 nM 8.80
CHEMBL2178257 Ki = 1.8 nM 8.74
CHEMBL2178266 Ki = 2.1 nM 8.68
CHEMBL2178807 Ki = 2.5 nM 8.60
CHEMBL2178253 Ki = 3.2 nM 8.49
CHEMBL2178252 Ki = 3.2 nM 8.49
CHEMBL2178247 Ki = 5.1 nM 8.29
CHEMBL2177122 Ki = 5.2 nM 8.28
CHEMBL2178260 Ki = 5.6 nM 8.25
CHEMBL2178249 Ki = 7.1 nM 8.15
CHEMBL2178250 Ki = 9.7 nM 8.01
CHEMBL2178806 Ki = 11.9 nM 7.92
CHEMBL2178261 Ki = 14.0 nM 7.85
CHEMBL2178248 Ki = 15.5 nM 7.81
CHEMBL2178263 Ki = 16.7 nM 7.78
CHEMBL2178256 Ki = 31.9 nM 7.50
CHEMBL2178262 Ki = 41.1 nM 7.39
CHEMBL2178264 Ki = 41.2 nM 7.38
CHEMBL2178259 Ki = 49.0 nM 7.31
CHEMBL2178265 Ki = 63.3 nM 7.20
CHEMBL2178251 Ki = 103.0 nM 6.99