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Assay Detail

CHEMBL800744

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Binding
Tested for inhibition against HIV-1 RT (used (poly)rC-(oligo)dG as the template)
ChEMBL ↗
59
Total Activities
59
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

Synthesis and evaluation of 2-pyridinone derivatives as HIV-1-specific reverse transcriptase inhibitors. 4. 3-[2-(Benzoxazol-2-yl)ethyl]-5-ethyl-6-methylpyridin-2(1H)-one and analogues.
Hoffman JM, Smith AM, Rooney CS, Fisher TE, Wai JS, Thomas CM, Bamberger DL, Barnes JL, Williams TM, Jones JH.
J Med Chem (1993) 36 : 953 -966
PubMed 7683054 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 59 6.56 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL171919 — — 1 7.96
CHEMBL368116 — — 1 7.89
CHEMBL177271 — — 1 7.85
CHEMBL99235 — — 1 7.85
CHEMBL176362 — — 1 7.82
CHEMBL175162 — — 1 7.82
CHEMBL268871 L-697661 — 1 7.70
CHEMBL83622 — — 1 7.64
CHEMBL172861 — — 1 7.62
CHEMBL329720 — — 1 7.55
CHEMBL174130 — — 1 7.54
CHEMBL174419 — — 1 7.52
CHEMBL172311 — — 1 7.52
CHEMBL177016 — — 1 7.48
CHEMBL176957 — — 1 7.47
CHEMBL367052 — — 1 7.43
CHEMBL171920 — — 1 7.41
CHEMBL176443 — — 1 7.40
CHEMBL172583 — — 1 7.37
CHEMBL176594 — — 1 7.32
CHEMBL173575 — — 1 7.28
CHEMBL176463 — — 1 7.24
CHEMBL176972 — — 1 7.21
CHEMBL173589 — — 1 7.08
CHEMBL176631 — — 1 7.06
CHEMBL174364 — — 1 7.01
CHEMBL98159 — — 1 6.89
CHEMBL426396 — — 1 6.77
CHEMBL177256 — — 1 6.76
CHEMBL177191 — — 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL171919 — IC50 = 11.0 nM 7.96
CHEMBL368116 — IC50 = 13.0 nM 7.89
CHEMBL99235 — IC50 = 14.0 nM 7.85
CHEMBL177271 — IC50 = 14.0 nM 7.85
CHEMBL176362 — IC50 = 15.0 nM 7.82
CHEMBL175162 — IC50 = 15.0 nM 7.82
CHEMBL268871 L-697661 IC50 = 20.0 nM 7.70
CHEMBL83622 — IC50 = 23.0 nM 7.64
CHEMBL172861 — IC50 = 24.0 nM 7.62
CHEMBL329720 — IC50 = 28.0 nM 7.55
CHEMBL174130 — IC50 = 29.0 nM 7.54
CHEMBL174419 — IC50 = 30.0 nM 7.52
CHEMBL172311 — IC50 = 30.0 nM 7.52
CHEMBL177016 — IC50 = 33.0 nM 7.48
CHEMBL176957 — IC50 = 34.0 nM 7.47
CHEMBL367052 — IC50 = 37.0 nM 7.43
CHEMBL171920 — IC50 = 39.0 nM 7.41
CHEMBL176443 — IC50 = 40.0 nM 7.40
CHEMBL172583 — IC50 = 43.0 nM 7.37
CHEMBL176594 — IC50 = 48.0 nM 7.32
CHEMBL173575 — IC50 = 52.0 nM 7.28
CHEMBL176463 — IC50 = 58.0 nM 7.24
CHEMBL176972 — IC50 = 62.0 nM 7.21
CHEMBL173589 — IC50 = 83.0 nM 7.08
CHEMBL176631 — IC50 = 88.0 nM 7.06
CHEMBL174364 — IC50 = 97.0 nM 7.01
CHEMBL98159 — IC50 = 130.0 nM 6.89
CHEMBL426396 — IC50 = 170.0 nM 6.77
CHEMBL177256 — IC50 = 172.0 nM 6.76
CHEMBL177191 — IC50 = 177.0 nM 6.75
CHEMBL174311 — IC50 = 191.0 nM 6.72
CHEMBL176637 — IC50 = 205.0 nM 6.69
CHEMBL415320 — IC50 = 210.0 nM 6.68
CHEMBL174953 — IC50 = 310.0 nM 6.51
CHEMBL95426 — IC50 = 370.0 nM 6.43
CHEMBL173635 — IC50 = 385.0 nM 6.42
CHEMBL177898 — IC50 = 442.0 nM 6.36
CHEMBL174267 — IC50 = 1100.0 nM 5.96
CHEMBL175089 — IC50 = 1250.0 nM 5.90
CHEMBL176814 — IC50 = 1400.0 nM 5.85
CHEMBL175531 — IC50 = 1700.0 nM 5.77
CHEMBL177192 — IC50 = 1850.0 nM 5.73
CHEMBL177174 — IC50 = 2100.0 nM 5.68
CHEMBL173529 — IC50 = 2450.0 nM 5.61
CHEMBL176587 — IC50 = 3000.0 nM 5.52
CHEMBL367204 — IC50 = 3400.0 nM 5.47
CHEMBL82439 — IC50 = 3700.0 nM 5.43
CHEMBL172773 — IC50 = 5400.0 nM 5.27
CHEMBL175037 — IC50 = 5900.0 nM 5.23
CHEMBL175235 — IC50 = 8400.0 nM 5.08