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Assay Detail

CHEMBL834476

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

Functional
Effective concentration of the compound to inhibit HIV-1 mutant K103N replication in HIV-infected MT-4 cells
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type MT4
Confidence 1 — Organism
Curated By Intermediate

Target

MT4 (CHEMBL388)
Type CELL-LINE
Organism Homo sapiens

Publication

From 4,5,6,7-tetrahydro-5-methylimidazo[4,5,1-jk](1,4)benzodiazepin-2(1H)-one (TIBO) to etravirine (TMC125): fifteen years of research on non-nucleoside inhibitors of HIV-1 reverse transcriptase.
De Corte BL.
J Med Chem (2005) 48 : 1689 -1696
PubMed 15771411 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 7.80 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL70517 1 9.40
CHEMBL308954 ETRAVIRINE 4.0 1 9.00
CHEMBL439757 1 9.00
CHEMBL70442 1 8.70
CHEMBL71728 1 8.52
CHEMBL72335 1 8.52
CHEMBL305803 1 8.52
CHEMBL73008 1 8.52
CHEMBL70663 DAPIVIRINE 3.0 1 8.40
CHEMBL71882 1 8.15
CHEMBL305838 1 8.10
CHEMBL74239 1 7.92
CHEMBL223228 EFAVIRENZ 4.0 1 7.40
CHEMBL307297 1 7.40
CHEMBL303457 1 6.23
CHEMBL37624 LOVIRIDE 2.0 1 5.89
CHEMBL593 DELAVIRDINE 4.0 1 5.60
CHEMBL57 NEVIRAPINE 4.0 1 5.20
CHEMBL74226 1 -
CHEMBL421112 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL70517 EC50 = 0.4 nM 9.40
CHEMBL308954 ETRAVIRINE EC50 = 1.0 nM 9.00
CHEMBL439757 EC50 = 1.0 nM 9.00
CHEMBL70442 EC50 = 2.0 nM 8.70
CHEMBL71728 EC50 = 3.0 nM 8.52
CHEMBL72335 EC50 = 3.0 nM 8.52
CHEMBL305803 EC50 = 3.0 nM 8.52
CHEMBL73008 EC50 = 3.0 nM 8.52
CHEMBL70663 DAPIVIRINE EC50 = 4.0 nM 8.40
CHEMBL71882 EC50 = 7.0 nM 8.15
CHEMBL305838 EC50 = 8.0 nM 8.10
CHEMBL74239 EC50 = 12.0 nM 7.92
CHEMBL223228 EFAVIRENZ EC50 = 40.0 nM 7.40
CHEMBL307297 EC50 = 40.0 nM 7.40
CHEMBL303457 EC50 = 590.0 nM 6.23
CHEMBL37624 LOVIRIDE EC50 = 1300.0 nM 5.89
CHEMBL593 DELAVIRDINE EC50 = 2500.0 nM 5.60
CHEMBL57 NEVIRAPINE EC50 = 6310.0 nM 5.20
CHEMBL74226 EC50 > 10000.0 nM -
CHEMBL421112 EC50 > 10000.0 nM -