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Assay Detail

CHEMBL4683032

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

Functional
Antiproliferative activity against human HL-60 cells assessed as cell growth inhibition after 72 hrs by trypan blue staining based cell counting assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HL-60
Confidence 1 — Organism
Curated By Autocuration

Target

HL-60 (CHEMBL383)
Type CELL-LINE
Organism Homo sapiens

Publication

A 18β-glycyrrhetinic acid conjugate with Vorinostat degrades HDAC3 and HDAC6 with improved antitumor effects.
Huang M,Xie X,Gong P,Wei Y,Du H,Xu Y,Xu Q,Jing Y,Zhao L
Eur J Med Chem (2020) 188 : 111991 -111991
PubMed 31883490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.53 6.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4749523 1 6.43
CHEMBL98 VORINOSTAT 4.0 1 6.38
CHEMBL4777978 1 6.14
CHEMBL412101 1 5.87
CHEMBL4764655 1 5.87
CHEMBL4799339 1 5.85
CHEMBL4764645 1 5.82
CHEMBL4747283 1 5.79
CHEMBL4798060 1 5.75
CHEMBL4780648 1 5.68
CHEMBL4756527 1 5.56
CHEMBL4795469 1 5.55
CHEMBL4798231 1 5.47
CHEMBL4786061 1 5.36
CHEMBL4798787 1 5.32
CHEMBL4786803 1 5.06
CHEMBL4787445 1 5.02
CHEMBL4750111 1 4.81
CHEMBL4779111 1 4.67
CHEMBL230006 ENOXOLONE 2.0 1 4.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4749523 IC50 = 370.0 nM 6.43
CHEMBL98 VORINOSTAT IC50 = 420.0 nM 6.38
CHEMBL4777978 IC50 = 720.0 nM 6.14
CHEMBL412101 IC50 = 1350.0 nM 5.87
CHEMBL4764655 IC50 = 1340.0 nM 5.87
CHEMBL4799339 IC50 = 1420.0 nM 5.85
CHEMBL4764645 IC50 = 1530.0 nM 5.82
CHEMBL4747283 IC50 = 1620.0 nM 5.79
CHEMBL4798060 IC50 = 1790.0 nM 5.75
CHEMBL4780648 IC50 = 2080.0 nM 5.68
CHEMBL4756527 IC50 = 2770.0 nM 5.56
CHEMBL4795469 IC50 = 2830.0 nM 5.55
CHEMBL4798231 IC50 = 3350.0 nM 5.47
CHEMBL4786061 IC50 = 4420.0 nM 5.36
CHEMBL4798787 IC50 = 4790.0 nM 5.32
CHEMBL4786803 IC50 = 8780.0 nM 5.06
CHEMBL4787445 IC50 = 9530.0 nM 5.02
CHEMBL4750111 IC50 = 15450.0 nM 4.81
CHEMBL4779111 IC50 = 21610.0 nM 4.67
CHEMBL230006 ENOXOLONE IC50 = 55280.0 nM 4.26