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Assay Detail

CHEMBL4397106

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

ADMET
Activation of non-specific gene expression in human J-Lat 10.6 cells harboring LTR driven GFP reporter co-expressing CMV driven RFP reporter assessed as CMV driven gene expression incubated for 48 hr by FACSCalibur flow cytometry
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification of 5-Substituted 2-Acylaminothiazoles That Activate Tat-Mediated Transcription in HIV-1 Latency Models.
Nguyen W, Jacobson J, Jarman KE, Jousset Sabroux H, Harty L, McMahon J, Lewin SR, Purcell DF, Sleebs BE.
J Med Chem (2019) 62 : 5148 -5175
PubMed 30973727 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 5.38 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL483254 PANOBINOSTAT 4.0 1 7.40
CHEMBL343448 ROMIDEPSIN 4.0 1 6.28
CHEMBL98 VORINOSTAT 4.0 1 5.72
CHEMBL4446565 1 5.70
CHEMBL4460170 1 5.20
CHEMBL4540359 1 4.89
CHEMBL4445805 1 4.75
CHEMBL4435131 1 4.72
CHEMBL4549436 1 4.55
CHEMBL4552693 1 4.54
CHEMBL4583543 1 -
CHEMBL4467303 1 -
CHEMBL4465202 1 -
CHEMBL2132936 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL483254 PANOBINOSTAT EC50 = 40.0 nM 7.40
CHEMBL343448 ROMIDEPSIN EC50 = 520.0 nM 6.28
CHEMBL98 VORINOSTAT EC50 = 1900.0 nM 5.72
CHEMBL4446565 EC50 = 2000.0 nM 5.70
CHEMBL4460170 EC50 = 6300.0 nM 5.20
CHEMBL4540359 EC50 = 13000.0 nM 4.89
CHEMBL4445805 EC50 = 18000.0 nM 4.75
CHEMBL4435131 EC50 = 19000.0 nM 4.72
CHEMBL4549436 EC50 = 28000.0 nM 4.55
CHEMBL4552693 EC50 = 29000.0 nM 4.54
CHEMBL4583543 EC50 > 40000.0 nM -
CHEMBL4467303 EC50 > 40000.0 nM -
CHEMBL4465202 EC50 > 40000.0 nM -
CHEMBL2132936 EC50 > 40000.0 nM -