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Assay Detail

CHEMBL4236283

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

Functional
Pro-apoptotic activity in human HUT78 cells after 18 hrs by caspase-Glo 3/7 assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HuT78
Confidence 1 — Organism
Curated By Intermediate

Target

HuT78 (CHEMBL613978)
Type CELL-LINE
Organism Homo sapiens

Publication

Squaramides as novel class I and IIB histone deacetylase inhibitors for topical treatment of cutaneous t-cell lymphoma.
Fournier JF, Bhurruth-Alcor Y, Musicki B, Aubert J, Aurelly M, Bouix-Peter C, Bouquet K, Chantalat L, Delorme M, Drean B, Duvert G, Fleury-Bregeot N, Gauthier B, Grisendi K, Harris CS, Hennequin LF, Isabet T, Joly F, Lafitte G, Millois C, Morgentin R, Pascau J, Piwnica D, Rival Y, Soulet C, Thoreau É, Tomas L.
Bioorg Med Chem Lett (2018) 28 : 2985 -2992
PubMed 30122227 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 38 7.43 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4239232 1 8.77
CHEMBL4241807 1 8.40
CHEMBL483254 PANOBINOSTAT 4.0 1 8.37
CHEMBL4237803 1 8.31
CHEMBL4250302 1 8.26
CHEMBL4251203 1 8.25
CHEMBL4242426 1 8.21
CHEMBL2105763 QUISINOSTAT 2.0 1 8.19
CHEMBL4241370 1 8.14
CHEMBL4246561 1 8.14
CHEMBL4242292 1 8.00
CHEMBL4237636 1 7.92
CHEMBL4250739 1 7.92
CHEMBL4240163 1 7.89
CHEMBL4240635 1 7.75
CHEMBL4249385 1 7.68
CHEMBL4245007 1 7.58
CHEMBL4248374 1 7.58
CHEMBL4247370 1 7.55
CHEMBL4251365 1 7.55
CHEMBL4246919 1 7.50
CHEMBL4238353 1 7.42
CHEMBL4244362 1 7.36
CHEMBL4242750 1 7.08
CHEMBL4244764 1 7.01
CHEMBL4251517 1 7.00
CHEMBL4241014 1 6.89
CHEMBL4245236 1 6.80
CHEMBL4241594 1 6.77
CHEMBL4244537 1 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4239232 EC50 = 1.7 nM 8.77
CHEMBL4241807 EC50 = 4.0 nM 8.40
CHEMBL483254 PANOBINOSTAT EC50 = 4.3 nM 8.37
CHEMBL4237803 EC50 = 4.9 nM 8.31
CHEMBL4250302 EC50 = 5.5 nM 8.26
CHEMBL4251203 EC50 = 5.6 nM 8.25
CHEMBL4242426 EC50 = 6.2 nM 8.21
CHEMBL2105763 QUISINOSTAT EC50 = 6.5 nM 8.19
CHEMBL4241370 EC50 = 7.3 nM 8.14
CHEMBL4246561 EC50 = 7.2 nM 8.14
CHEMBL4242292 EC50 = 10.0 nM 8.00
CHEMBL4237636 EC50 = 12.0 nM 7.92
CHEMBL4250739 EC50 = 12.0 nM 7.92
CHEMBL4240163 EC50 = 13.0 nM 7.89
CHEMBL4240635 EC50 = 18.0 nM 7.75
CHEMBL4249385 EC50 = 21.0 nM 7.68
CHEMBL4245007 EC50 = 26.0 nM 7.58
CHEMBL4248374 EC50 = 26.0 nM 7.58
CHEMBL4251365 EC50 = 28.0 nM 7.55
CHEMBL4247370 EC50 = 28.0 nM 7.55
CHEMBL4246919 EC50 = 32.0 nM 7.50
CHEMBL4238353 EC50 = 38.0 nM 7.42
CHEMBL4244362 EC50 = 44.0 nM 7.36
CHEMBL4242750 EC50 = 84.0 nM 7.08
CHEMBL4244764 EC50 = 98.0 nM 7.01
CHEMBL4251517 EC50 = 100.0 nM 7.00
CHEMBL4241014 EC50 = 130.0 nM 6.89
CHEMBL4245236 EC50 = 160.0 nM 6.80
CHEMBL4241594 EC50 = 170.0 nM 6.77
CHEMBL4244537 EC50 = 220.0 nM 6.66
CHEMBL4248346 EC50 = 270.0 nM 6.57
CHEMBL4242086 EC50 = 280.0 nM 6.55
CHEMBL4238532 EC50 = 280.0 nM 6.55
CHEMBL4244350 EC50 = 290.0 nM 6.54
CHEMBL4241251 EC50 = 290.0 nM 6.54
CHEMBL98 VORINOSTAT EC50 = 290.0 nM 6.54
CHEMBL4245840 EC50 = 560.0 nM 6.25
CHEMBL4249281 EC50 = 1100.0 nM 5.96