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Assay Detail

CHEMBL802597

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Binding
Inhibitory activity against HIV-1 Reverse Transcriptase with rCdG as the template primer
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Human immunodeficiency virus type 1 reverse transcriptase (CHEMBL247)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

The biological effects of structural variation at the meta position of the aromatic rings and at the end of the alkenyl chain in the alkenyldiarylmethane series of non-nucleoside reverse transcriptase inhibitors.
Xu G, Micklatcher M, Silvestri MA, Hartman TL, Burrier J, Osterling MC, Wargo H, Turpin JA, Buckheit RW, Cushman M.
J Med Chem (2001) 44 : 4092 -4113
PubMed 11708913 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 41 5.49 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL133772 1 7.80
CHEMBL131518 1 6.74
CHEMBL129835 1 6.63
CHEMBL107200 1 6.52
CHEMBL340869 1 6.45
CHEMBL58542 1 6.42
CHEMBL131761 1 6.30
CHEMBL133010 1 6.16
CHEMBL335768 1 6.00
CHEMBL335037 1 5.71
CHEMBL132489 1 5.62
CHEMBL133393 1 5.53
CHEMBL63497 1 5.50
CHEMBL133678 1 5.35
CHEMBL130316 1 5.31
CHEMBL130336 1 5.25
CHEMBL325757 1 5.22
CHEMBL264639 1 5.15
CHEMBL326205 1 5.08
CHEMBL323016 1 5.04
CHEMBL132790 1 5.02
CHEMBL131432 1 5.00
CHEMBL305535 1 4.96
CHEMBL106414 1 4.53
CHEMBL323276 1 4.22
CHEMBL133842 1 4.18
CHEMBL323259 1 4.15
CHEMBL108267 1 4.00
CHEMBL130934 1 -
CHEMBL339176 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL133772 IC50 = 16.0 nM 7.80
CHEMBL131518 IC50 = 181.0 nM 6.74
CHEMBL129835 IC50 = 233.0 nM 6.63
CHEMBL107200 IC50 = 300.0 nM 6.52
CHEMBL340869 IC50 = 359.0 nM 6.45
CHEMBL58542 IC50 = 380.0 nM 6.42
CHEMBL131761 IC50 = 499.0 nM 6.30
CHEMBL133010 IC50 = 687.0 nM 6.16
CHEMBL335768 IC50 = 1000.0 nM 6.00
CHEMBL335037 IC50 = 1930.0 nM 5.71
CHEMBL132489 IC50 = 2390.0 nM 5.62
CHEMBL133393 IC50 = 2950.0 nM 5.53
CHEMBL63497 IC50 = 3200.0 nM 5.50
CHEMBL133678 IC50 = 4430.0 nM 5.35
CHEMBL130316 IC50 = 4930.0 nM 5.31
CHEMBL130336 IC50 = 5650.0 nM 5.25
CHEMBL325757 IC50 = 6000.0 nM 5.22
CHEMBL264639 IC50 = 7120.0 nM 5.15
CHEMBL326205 IC50 = 8300.0 nM 5.08
CHEMBL323016 IC50 = 9150.0 nM 5.04
CHEMBL132790 IC50 = 9470.0 nM 5.02
CHEMBL131432 IC50 = 10000.0 nM 5.00
CHEMBL305535 IC50 = 11000.0 nM 4.96
CHEMBL106414 IC50 = 29700.0 nM 4.53
CHEMBL323276 IC50 = 60400.0 nM 4.22
CHEMBL133842 IC50 = 65400.0 nM 4.18
CHEMBL323259 IC50 = 70800.0 nM 4.15
CHEMBL108267 IC50 = 99000.0 nM 4.00
CHEMBL133685 IC50 > 100000.0 nM -
CHEMBL131699 IC50 > 100000.0 nM -
CHEMBL133395 IC50 > 100000.0 nM -
CHEMBL336737 IC50 > 100000.0 nM -
CHEMBL110175 IC50 > 100000.0 nM -
CHEMBL130041 IC50 > 200000.0 nM -
CHEMBL110224 IC50 = 258000.0 nM -
CHEMBL130984 IC50 > 100000.0 nM -
CHEMBL428685 IC50 < 1000.0 nM -
CHEMBL106554 IC50 > 100000.0 nM -
CHEMBL131674 IC50 > 100000.0 nM -
CHEMBL339176 IC50 > 100000.0 nM -
CHEMBL130934 IC50 > 100000.0 nM -