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Assay Detail

CHEMBL4669384

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Binding
Inhibition of Class 1 HDAC in VSV-G-pseudotyped HIV infected human 2C4 cell Jurkat model assessed as reactivation of HIV latency in presence of 0.1% NHS by fluorescent reporter gene assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 2C4
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Class 1 histone deacetylase (CHEMBL4523988)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Development of a selective HDAC inhibitor aimed at reactivating the HIV latent reservoir.
Clausen DJ,Liu J,Yu W,Duffy JL,Chung CC,Myers RW,Klein DJ,Fells J,Holloway K,Wu J,Wu G,Howell BJ,Barnard RJO,Kozlowski J
Bioorg Med Chem Lett (2020) 30 : 127367 -127367
PubMed 32738976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 24 6.33 7.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4746782 1 7.11
CHEMBL4759693 1 6.98
CHEMBL4797893 1 6.97
CHEMBL4742036 1 6.81
CHEMBL4759472 1 6.79
CHEMBL4748244 1 6.78
CHEMBL4785376 1 6.71
CHEMBL4788911 1 6.63
CHEMBL4761973 1 6.61
CHEMBL4760209 1 6.59
CHEMBL4776685 1 6.53
CHEMBL4765128 1 6.26
CHEMBL4746267 1 6.25
CHEMBL4739902 1 6.25
CHEMBL4782188 1 6.24
CHEMBL4781191 1 6.11
CHEMBL4761318 1 5.94
CHEMBL4797194 1 5.91
CHEMBL4754763 1 5.81
CHEMBL4756752 1 5.79
CHEMBL4741084 1 5.76
CHEMBL4796175 1 5.74
CHEMBL4750027 1 5.67
CHEMBL4793558 1 5.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4746782 EC50 = 77.0 nM 7.11
CHEMBL4759693 EC50 = 105.0 nM 6.98
CHEMBL4797893 EC50 = 107.0 nM 6.97
CHEMBL4742036 EC50 = 154.0 nM 6.81
CHEMBL4759472 EC50 = 161.0 nM 6.79
CHEMBL4748244 EC50 = 166.0 nM 6.78
CHEMBL4785376 EC50 = 193.0 nM 6.71
CHEMBL4788911 EC50 = 233.0 nM 6.63
CHEMBL4761973 EC50 = 247.0 nM 6.61
CHEMBL4760209 EC50 = 254.0 nM 6.59
CHEMBL4776685 EC50 = 294.0 nM 6.53
CHEMBL4765128 EC50 = 548.0 nM 6.26
CHEMBL4746267 EC50 = 566.0 nM 6.25
CHEMBL4739902 EC50 = 558.0 nM 6.25
CHEMBL4782188 EC50 = 570.0 nM 6.24
CHEMBL4781191 EC50 = 775.0 nM 6.11
CHEMBL4761318 EC50 = 1142.0 nM 5.94
CHEMBL4797194 EC50 = 1233.0 nM 5.91
CHEMBL4754763 EC50 = 1564.0 nM 5.81
CHEMBL4756752 EC50 = 1605.0 nM 5.79
CHEMBL4741084 EC50 = 1731.0 nM 5.76
CHEMBL4796175 EC50 = 1834.0 nM 5.74
CHEMBL4750027 EC50 = 2112.0 nM 5.67
CHEMBL4793558 EC50 = 2729.0 nM 5.56