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Assay Detail

CHEMBL712399

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

Functional
Dose required to achieve 50% protection of MT-4 cells from HIV-1(IIIB) induced cytopathogenicity, determined by MIT method.
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type MT4
Confidence 1 — Organism
Curated By Expert

Target

MT4 (CHEMBL388)
Type CELL-LINE
Organism Homo sapiens

Publication

Novel 1,1,3-trioxo-2H,4H-thieno[3,4-e][1,2,4]thiadiazine derivatives as non-nucleoside reverse transcriptase inhibitors that inhibit human immunodeficiency virus type 1 replication.
Arranz E, Díaz JA, Ingate ST, Witvrouw M, Pannecouque C, Balzarini J, De Clercq E, Vega S.
J Med Chem (1998) 41 : 4109 -4117
PubMed 9767646 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 40 5.96 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 9.15
CHEMBL57 NEVIRAPINE 4.0 1 7.52
CHEMBL130390 1 7.30
CHEMBL129949 1 7.05
CHEMBL337392 1 7.05
CHEMBL133626 1 7.00
CHEMBL336723 1 7.00
CHEMBL337668 1 6.70
CHEMBL131152 1 6.52
CHEMBL133052 1 6.40
CHEMBL132556 1 6.10
CHEMBL132150 1 6.05
CHEMBL334614 1 6.00
CHEMBL335321 1 5.96
CHEMBL133478 1 5.85
CHEMBL336513 1 5.68
CHEMBL336622 1 5.66
CHEMBL133679 1 5.60
CHEMBL435395 1 5.57
CHEMBL131848 1 5.52
CHEMBL334862 1 5.44
CHEMBL132792 1 5.35
CHEMBL337397 1 5.14
CHEMBL424270 1 5.13
CHEMBL133057 1 5.12
CHEMBL335286 1 5.08
CHEMBL424447 1 5.07
CHEMBL130613 1 4.96
CHEMBL130220 1 4.69
CHEMBL334895 1 4.61

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE EC50 = 0.7 nM 9.15
CHEMBL57 NEVIRAPINE EC50 = 30.0 nM 7.52
CHEMBL130390 EC50 = 50.0 nM 7.30
CHEMBL129949 EC50 = 90.0 nM 7.05
CHEMBL337392 EC50 = 90.0 nM 7.05
CHEMBL133626 EC50 = 100.0 nM 7.00
CHEMBL336723 EC50 = 100.0 nM 7.00
CHEMBL337668 EC50 = 200.0 nM 6.70
CHEMBL131152 EC50 = 300.0 nM 6.52
CHEMBL133052 EC50 = 400.0 nM 6.40
CHEMBL132556 EC50 = 800.0 nM 6.10
CHEMBL132150 EC50 = 900.0 nM 6.05
CHEMBL334614 EC50 = 1000.0 nM 6.00
CHEMBL335321 EC50 = 1100.0 nM 5.96
CHEMBL133478 EC50 = 1400.0 nM 5.85
CHEMBL336513 EC50 = 2100.0 nM 5.68
CHEMBL336622 EC50 = 2200.0 nM 5.66
CHEMBL133679 EC50 = 2500.0 nM 5.60
CHEMBL435395 EC50 = 2700.0 nM 5.57
CHEMBL131848 EC50 = 3000.0 nM 5.52
CHEMBL334862 EC50 = 3600.0 nM 5.44
CHEMBL132792 EC50 = 4500.0 nM 5.35
CHEMBL337397 EC50 = 7300.0 nM 5.14
CHEMBL424270 EC50 = 7400.0 nM 5.13
CHEMBL133057 EC50 = 7600.0 nM 5.12
CHEMBL335286 EC50 = 8300.0 nM 5.08
CHEMBL424447 EC50 = 8600.0 nM 5.07
CHEMBL130613 EC50 = 10900.0 nM 4.96
CHEMBL130220 EC50 = 20500.0 nM 4.69
CHEMBL334895 EC50 = 24500.0 nM 4.61
CHEMBL134199 EC50 = 41400.0 nM 4.38
CHEMBL133277 EC50 > 498500.0 nM -
CHEMBL336838 EC50 > 417000.0 nM -
CHEMBL132132 EC50 > 273000.0 nM -
CHEMBL133956 EC50 > 320600.0 nM -
CHEMBL424626 EC50 > 446300.0 nM -
CHEMBL133056 EC50 > 527500.0 nM -
CHEMBL134034 EC50 > 403000.0 nM -
CHEMBL134035 EC50 > 811000.0 nM -
CHEMBL132831 EC50 > 74100.0 nM -