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Assay Detail

CHEMBL3877398

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

Functional
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MDA-MB-231
Confidence 1 — Organism
Curated By Autocuration

Publication

Design and Synthesis of Janus Kinase 2 (JAK2) and Histone Deacetlyase (HDAC) Bispecific Inhibitors Based on Pacritinib and Evidence of Dual Pathway Inhibition in Hematological Cell Lines.
Yang EG, Mustafa N, Tan EC, Poulsen A, Ramanujulu PM, Chng WJ, Yen JJ, Dymock BW.
J Med Chem (2016) 59 : 8233 -8262
PubMed 27541357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.01 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL98 VORINOSTAT 4.0 1 5.92
CHEMBL3917405 1 5.84
CHEMBL2035187 PACRITINIB 4.0 1 5.61
CHEMBL3961053 1 5.47
CHEMBL3972157 1 5.46
CHEMBL3942555 1 5.23
CHEMBL3945293 1 5.19
CHEMBL3951291 1 5.09
CHEMBL3915689 1 5.06
CHEMBL2018302 TUBASTATIN A 1 4.98
CHEMBL3893970 1 4.97
CHEMBL3920872 1 4.92
CHEMBL3980203 1 4.90
CHEMBL3943650 1 4.77
CHEMBL3892860 1 4.70
CHEMBL3982857 1 4.67
CHEMBL3911929 1 4.59
CHEMBL3954183 1 4.34
CHEMBL3981879 1 4.27
CHEMBL3962918 1 4.27
CHEMBL3952364 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL98 VORINOSTAT IC50 = 1190.0 nM 5.92
CHEMBL3917405 IC50 = 1430.0 nM 5.84
CHEMBL2035187 PACRITINIB IC50 = 2430.0 nM 5.61
CHEMBL3961053 IC50 = 3410.0 nM 5.47
CHEMBL3972157 IC50 = 3430.0 nM 5.46
CHEMBL3942555 IC50 = 5910.0 nM 5.23
CHEMBL3945293 IC50 = 6440.0 nM 5.19
CHEMBL3951291 IC50 = 8070.0 nM 5.09
CHEMBL3915689 IC50 = 8690.0 nM 5.06
CHEMBL2018302 TUBASTATIN A IC50 = 10400.0 nM 4.98
CHEMBL3893970 IC50 = 10700.0 nM 4.97
CHEMBL3920872 IC50 = 12000.0 nM 4.92
CHEMBL3980203 IC50 = 12700.0 nM 4.90
CHEMBL3943650 IC50 = 17100.0 nM 4.77
CHEMBL3892860 IC50 = 19900.0 nM 4.70
CHEMBL3982857 IC50 = 21400.0 nM 4.67
CHEMBL3911929 IC50 = 25900.0 nM 4.59
CHEMBL3954183 IC50 = 46000.0 nM 4.34
CHEMBL3981879 IC50 = 53500.0 nM 4.27
CHEMBL3962918 IC50 = 54200.0 nM 4.27
CHEMBL3952364 IC50 > 50000.0 nM -