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Assay Detail

CHEMBL4052442

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

Binding
Inhibition of human ERG expressed in HEK293 cells by patch clamp method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Structure-Based Optimization of Thiophene[3,2-d]pyrimidine Derivatives as Potent HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Improved Potency against Resistance-Associated Variants.
Kang D, Fang Z, Huang B, Lu X, Zhang H, Xu H, Huo Z, Zhou Z, Yu Z, Meng Q, Wu G, Ding X, Tian Y, Daelemans D, De Clercq E, Pannecouque C, Zhan P, Liu X.
J Med Chem (2017) 60 : 4424 -4443
PubMed 28481112 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.20 7.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17157 TERFENADINE 4.0 1 7.66
CHEMBL4094163 1 6.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17157 TERFENADINE IC50 = 22.0 nM 7.66
CHEMBL4094163 IC50 = 186.0 nM 6.73