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Assay Detail

CHEMBL4841939

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Functional
Antiviral activity against HIV-1 infected in MT4 cells assessed as reduction in virus-induced cytopathic effect preincubated for 1 hr followed by viral infection and measured after 5 days by XTT assay
ChEMBL ↗
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT4
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378) ↗
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Discovery of Modified Amidate (ProTide) Prodrugs of Tenofovir with Enhanced Antiviral Properties.
Kalčic F, Zgarbová M, Hodek J, Chalupský K, Dračínský M, Dvořáková A, Strmeň T, Šebestík J, Baszczyňski O, Weber J, Mertlíková-Kaiserová H, Janeba Z.
J Med Chem (2021) 64 : 16425 -16449
PubMed 34713696 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 51 8.03 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4873511 — — 1 11.00
CHEMBL4853566 — — 1 10.22
CHEMBL4848092 — — 1 10.15
CHEMBL4849286 — — 1 9.82
CHEMBL4877392 — — 1 9.55
CHEMBL4879329 — — 1 9.48
CHEMBL4868959 — — 1 9.44
CHEMBL4875146 — — 1 9.40
CHEMBL4846072 — — 1 9.25
CHEMBL4857530 — — 1 9.22
CHEMBL4849197 — — 1 9.17
CHEMBL4861112 — — 1 9.17
CHEMBL4869422 — — 1 9.05
CHEMBL4859604 — — 1 8.80
CHEMBL4855770 — — 1 8.74
CHEMBL4859981 — — 1 8.48
CHEMBL4876528 — — 1 8.47
CHEMBL2364637 TENOFOVIR ALAFENAMIDE FUMARATE 4.0 1 8.19
CHEMBL4870001 — — 1 8.08
CHEMBL4862475 — — 1 8.05
CHEMBL4870172 — — 1 8.02
CHEMBL4869513 — — 1 8.00
CHEMBL4865643 — — 1 7.96
CHEMBL4869095 — — 1 7.96
CHEMBL4863401 — — 1 7.89
CHEMBL4876052 — — 1 7.89
CHEMBL4854086 — — 1 7.80
CHEMBL4846576 — — 1 7.80
CHEMBL4862081 — — 1 7.80
CHEMBL4853300 — — 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4873511 — EC50 = 0.01 nM 11.00
CHEMBL4853566 — EC50 = 0.06 nM 10.22
CHEMBL4848092 — EC50 = 0.07 nM 10.15
CHEMBL4849286 — EC50 = 0.15 nM 9.82
CHEMBL4877392 — EC50 = 0.28 nM 9.55
CHEMBL4879329 — EC50 = 0.33 nM 9.48
CHEMBL4868959 — EC50 = 0.36 nM 9.44
CHEMBL4875146 — EC50 = 0.4 nM 9.40
CHEMBL4846072 — EC50 = 0.56 nM 9.25
CHEMBL4857530 — EC50 = 0.6 nM 9.22
CHEMBL4849197 — EC50 = 0.68 nM 9.17
CHEMBL4861112 — EC50 = 0.67 nM 9.17
CHEMBL4869422 — EC50 = 0.9 nM 9.05
CHEMBL4859604 — EC50 = 1.6 nM 8.80
CHEMBL4855770 — EC50 = 1.8 nM 8.74
CHEMBL4859981 — EC50 = 3.3 nM 8.48
CHEMBL4876528 — EC50 = 3.4 nM 8.47
CHEMBL2364637 TENOFOVIR ALAFENAMIDE FUMARATE EC50 = 6.4 nM 8.19
CHEMBL4870001 — EC50 = 8.4 nM 8.08
CHEMBL4862475 — EC50 = 9.0 nM 8.05
CHEMBL4870172 — EC50 = 9.6 nM 8.02
CHEMBL4869513 — EC50 = 10.0 nM 8.00
CHEMBL4865643 — EC50 = 11.0 nM 7.96
CHEMBL4869095 — EC50 = 11.0 nM 7.96
CHEMBL4876052 — EC50 = 13.0 nM 7.89
CHEMBL4863401 — EC50 = 13.0 nM 7.89
CHEMBL4854086 — EC50 = 16.0 nM 7.80
CHEMBL4846576 — EC50 = 16.0 nM 7.80
CHEMBL4862081 — EC50 = 16.0 nM 7.80
CHEMBL4853300 — EC50 = 16.0 nM 7.80
CHEMBL4864042 — EC50 = 17.0 nM 7.77
CHEMBL4867245 — EC50 = 20.0 nM 7.70
CHEMBL4847679 — EC50 = 21.0 nM 7.68
CHEMBL4875800 — EC50 = 23.0 nM 7.64
CHEMBL4870111 — EC50 = 27.0 nM 7.57
CHEMBL4869886 — EC50 = 30.0 nM 7.52
CHEMBL4879191 — EC50 = 36.0 nM 7.44
CHEMBL4849428 — EC50 = 38.0 nM 7.42
CHEMBL4871257 — EC50 = 48.0 nM 7.32
CHEMBL4874018 — EC50 = 50.0 nM 7.30
CHEMBL4873059 — EC50 = 72.0 nM 7.14
CHEMBL4876334 — EC50 = 84.0 nM 7.08
CHEMBL4859319 — EC50 = 150.0 nM 6.82
CHEMBL4850548 — EC50 = 350.0 nM 6.46
CHEMBL4872816 — EC50 = 470.0 nM 6.33
CHEMBL4863664 — EC50 = 540.0 nM 6.27
CHEMBL4845876 — EC50 = 650.0 nM 6.19
CHEMBL4877971 — EC50 = 720.0 nM 6.14
CHEMBL4855762 — EC50 = 2200.0 nM 5.66
CHEMBL4862664 — EC50 = 2500.0 nM 5.60