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Assay Detail

CHEMBL4714136

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

Functional
Growth inhibition of human UKE-1 cells incubated for 72 hrs by Cell-titer blue assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type UKE-1
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structural Insights into JAK2 Inhibition by Ruxolitinib, Fedratinib, and Derivatives Thereof.
Davis RR,Li B,Yun SY,Chan A,Nareddy P,Gunawan S,Ayaz M,Lawrence HR,Reuther GW,Lawrence NJ,Schönbrunn E
J Med Chem (2021) 64 : 2228 -2241
PubMed 33570945 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 6.20 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1789941 RUXOLITINIB 4.0 1 7.00
CHEMBL4744236 1 6.82
CHEMBL2105759 BARICITINIB 4.0 1 6.72
CHEMBL4785050 1 6.70
CHEMBL4762807 1 6.68
CHEMBL4760892 1 6.50
CHEMBL2002099 1 6.42
CHEMBL4745155 1 6.21
CHEMBL1287853 FEDRATINIB 4.0 1 6.18
CHEMBL221959 TOFACITINIB 4.0 1 6.04
CHEMBL1287854 1 5.98
CHEMBL4788363 1 5.66
CHEMBL4750568 1 5.50
CHEMBL4753959 1 5.35
CHEMBL4743499 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1789941 RUXOLITINIB IC50 = 100.0 nM 7.00
CHEMBL4744236 IC50 = 150.0 nM 6.82
CHEMBL2105759 BARICITINIB IC50 = 190.0 nM 6.72
CHEMBL4785050 IC50 = 200.0 nM 6.70
CHEMBL4762807 IC50 = 210.0 nM 6.68
CHEMBL4760892 IC50 = 320.0 nM 6.50
CHEMBL2002099 IC50 = 380.0 nM 6.42
CHEMBL4745155 IC50 = 620.0 nM 6.21
CHEMBL1287853 FEDRATINIB IC50 = 660.0 nM 6.18
CHEMBL221959 TOFACITINIB IC50 = 910.0 nM 6.04
CHEMBL1287854 IC50 = 1040.0 nM 5.98
CHEMBL4788363 IC50 = 2200.0 nM 5.66
CHEMBL4750568 IC50 = 3200.0 nM 5.50
CHEMBL4753959 IC50 = 4500.0 nM 5.35
CHEMBL4743499 IC50 = 6300.0 nM 5.20