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Assay Detail

CHEMBL4431271

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Functional
Antiproliferative activity against HEL cells harboring JAK2 V617F mutant after 48 hrs by MTT assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEL
Confidence 1 — Organism
Curated By Autocuration

Target

HEL (CHEMBL613888)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, Synthesis, and Antitumor Evaluation of 4-Amino-(1<i>H</i>)-pyrazole Derivatives as JAKs Inhibitors.
Liang X, Zang J, Zhu M, Gao Q, Wang B, Xu W, Zhang Y.
ACS Med Chem Lett (2016) 7 : 950 -955
PubMed 27774135 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.71 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4448847 1 6.46
CHEMBL4453646 1 5.97
CHEMBL4439885 1 5.93
CHEMBL4459309 1 5.91
CHEMBL4474915 1 5.82
CHEMBL4476622 1 5.75
CHEMBL1789941 RUXOLITINIB 4.0 1 5.58
CHEMBL4555319 1 5.40
CHEMBL4537769 1 5.23
CHEMBL4583672 1 5.01
CHEMBL4483021 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4448847 IC50 = 350.0 nM 6.46
CHEMBL4453646 IC50 = 1080.0 nM 5.97
CHEMBL4439885 IC50 = 1180.0 nM 5.93
CHEMBL4459309 IC50 = 1240.0 nM 5.91
CHEMBL4474915 IC50 = 1530.0 nM 5.82
CHEMBL4476622 IC50 = 1760.0 nM 5.75
CHEMBL1789941 RUXOLITINIB IC50 = 2620.0 nM 5.58
CHEMBL4555319 IC50 = 3960.0 nM 5.40
CHEMBL4537769 IC50 = 5930.0 nM 5.23
CHEMBL4583672 IC50 = 9710.0 nM 5.01
CHEMBL4483021 IC50 - -