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Assay Detail

CHEMBL655350

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Functional
Effective concentration required to achieve 50% inhibition of HIV-1 LAI replication in human T4 lymphoblastoid CEM-SS cells.
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type CEM-SS
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 "AZT-HEPT", "AZT-pyridinone", and "ddC-HEPT" conjugates as inhibitors of HIV reverse transcriptase.
Pontikis R, Dollé V, Guillaumel J, Dechaux E, Note R, Nguyen CH, Legraverend M, Bisagni E, Aubertin AM, Grierson DS, Monneret C.
J Med Chem (2000) 43 : 1927 -1939
PubMed 10821705 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 27 5.71 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129 ZIDOVUDINE 4.0 1 8.70
CHEMBL57733 1 7.77
CHEMBL58213 1 7.60
CHEMBL853 ZALCITABINE 4.0 1 7.51
CHEMBL20610 1 6.37
CHEMBL417227 1 6.14
CHEMBL56328 1 6.10
CHEMBL440482 1 5.77
CHEMBL58914 1 5.55
CHEMBL58497 1 5.50
CHEMBL57161 1 5.48
CHEMBL418119 1 5.35
CHEMBL417953 1 5.11
CHEMBL58653 1 4.70
CHEMBL57301 1 4.62
CHEMBL57590 1 4.60
CHEMBL301685 1 4.48
CHEMBL292392 1 4.38
CHEMBL57929 1 4.24
CHEMBL418294 1 4.16
CHEMBL58891 1 -
CHEMBL300607 1 -
CHEMBL57313 1 -
CHEMBL418118 1 -
CHEMBL262003 1 -
CHEMBL60873 1 -
CHEMBL59514 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129 ZIDOVUDINE EC50 = 2.0 nM 8.70
CHEMBL57733 EC50 = 17.0 nM 7.77
CHEMBL58213 EC50 = 25.0 nM 7.60
CHEMBL853 ZALCITABINE EC50 = 31.0 nM 7.51
CHEMBL20610 EC50 = 430.0 nM 6.37
CHEMBL417227 EC50 = 720.0 nM 6.14
CHEMBL56328 EC50 = 800.0 nM 6.10
CHEMBL440482 EC50 = 1700.0 nM 5.77
CHEMBL58914 EC50 = 2800.0 nM 5.55
CHEMBL58497 EC50 = 3200.0 nM 5.50
CHEMBL57161 EC50 = 3300.0 nM 5.48
CHEMBL418119 EC50 = 4500.0 nM 5.35
CHEMBL417953 EC50 = 7800.0 nM 5.11
CHEMBL58653 EC50 = 20000.0 nM 4.70
CHEMBL57301 EC50 = 24000.0 nM 4.62
CHEMBL57590 EC50 = 25000.0 nM 4.60
CHEMBL301685 EC50 = 33000.0 nM 4.48
CHEMBL292392 EC50 = 42000.0 nM 4.38
CHEMBL57929 EC50 = 58000.0 nM 4.24
CHEMBL418294 EC50 = 70000.0 nM 4.16
CHEMBL58891 EC50 > 100000.0 nM -
CHEMBL300607 EC50 > 100000.0 nM -
CHEMBL57313 EC50 > 100000.0 nM -
CHEMBL418118 EC50 > 10000.0 nM -
CHEMBL262003 EC50 > 100000.0 nM -
CHEMBL60873 EC50 > 10000.0 nM -
CHEMBL59514 EC50 > 10000.0 nM -