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Assay Detail

CHEMBL895180

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Binding
Inhibition of HIV1 reverse transcriptase
39
Total Activities
39
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 Autocuration

Target

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

Publication

Synthesis and biological evaluation of alkenyldiarylmethane HIV-1 non-nucleoside reverse transcriptase inhibitors that possess increased hydrolytic stability.
Cullen MD, Deng BL, Hartman TL, Watson KM, Buckheit RW, Pannecouque C, Clercq ED, Cushman M.
J Med Chem (2007) 50 : 4854 -4867
PubMed 17803290 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 5.25 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL226735 1 7.70
CHEMBL294840 1 6.52
CHEMBL107200 1 6.52
CHEMBL243068 1 6.41
CHEMBL231473 1 6.35
CHEMBL387567 1 6.33
CHEMBL231274 1 6.28
CHEMBL244780 1 6.05
CHEMBL231470 1 6.04
CHEMBL243277 1 6.00
CHEMBL244781 1 5.58
CHEMBL231275 1 5.50
CHEMBL387804 1 5.28
CHEMBL244999 1 5.20
CHEMBL231072 1 5.17
CHEMBL243067 1 5.13
CHEMBL231377 1 5.11
CHEMBL245218 1 5.11
CHEMBL242843 1 5.11
CHEMBL438127 1 5.04
CHEMBL244998 1 5.03
CHEMBL243066 1 4.62
CHEMBL555376 1 4.54
CHEMBL242845 1 4.50
CHEMBL398201 1 4.48
CHEMBL231375 1 4.44
CHEMBL230966 1 4.32
CHEMBL3706913 1 4.28
CHEMBL398202 1 4.26
CHEMBL255525 1 4.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL226735 IC50 = 20.0 nM 7.70
CHEMBL294840 IC50 = 300.0 nM 6.52
CHEMBL107200 IC50 = 300.0 nM 6.52
CHEMBL243068 IC50 = 390.0 nM 6.41
CHEMBL231473 IC50 = 450.0 nM 6.35
CHEMBL387567 IC50 = 470.0 nM 6.33
CHEMBL231274 IC50 = 520.0 nM 6.28
CHEMBL244780 IC50 = 900.0 nM 6.05
CHEMBL231470 IC50 = 910.0 nM 6.04
CHEMBL243277 IC50 = 1000.0 nM 6.00
CHEMBL244781 IC50 = 2600.0 nM 5.58
CHEMBL231275 IC50 = 3200.0 nM 5.50
CHEMBL387804 IC50 = 5200.0 nM 5.28
CHEMBL244999 IC50 = 6300.0 nM 5.20
CHEMBL231072 IC50 = 6700.0 nM 5.17
CHEMBL243067 IC50 = 7400.0 nM 5.13
CHEMBL231377 IC50 = 7700.0 nM 5.11
CHEMBL245218 IC50 = 7700.0 nM 5.11
CHEMBL242843 IC50 = 7700.0 nM 5.11
CHEMBL438127 IC50 = 9200.0 nM 5.04
CHEMBL244998 IC50 = 9300.0 nM 5.03
CHEMBL243066 IC50 = 24000.0 nM 4.62
CHEMBL555376 IC50 = 29000.0 nM 4.54
CHEMBL242845 IC50 = 32000.0 nM 4.50
CHEMBL398201 IC50 = 33000.0 nM 4.48
CHEMBL231375 IC50 = 36000.0 nM 4.44
CHEMBL230966 IC50 = 48000.0 nM 4.32
CHEMBL3706913 IC50 = 53000.0 nM 4.28
CHEMBL398202 IC50 = 55000.0 nM 4.26
CHEMBL255525 IC50 = 67000.0 nM 4.17
CHEMBL242844 IC50 = 71000.0 nM 4.15
CHEMBL396233 IC50 = 90000.0 nM 4.05
CHEMBL3706914 IC50 = 95000.0 nM 4.02
CHEMBL429286 IC50 > 100000.0 nM -
CHEMBL231175 IC50 > 100000.0 nM -
CHEMBL231376 IC50 > 100000.0 nM -
CHEMBL241996 IC50 > 100000.0 nM -
CHEMBL57 NEVIRAPINE IC50 - -
CHEMBL223228 EFAVIRENZ IC50 - -