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Assay Detail

CHEMBL694657

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Tested in vitro against HIV-1 LAI from MT-4 cells using MTT assay
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT4
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

Syntheses of 4'-C-ethynyl-beta-D-arabino- and 4'-C-ethynyl-2'-deoxy-beta-D-ribo-pentofuranosylpyrimidines and -purines and evaluation of their anti-HIV activity.
Ohrui H, Kohgo S, Kitano K, Sakata S, Kodama E, Yoshimura K, Matsuoka M, Shigeta S, Mitsuya H.
J Med Chem (2000) 43 : 4516 -4525
PubMed 11087576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 7.40 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2368072 1 9.52
CHEMBL2012671 1 8.85
CHEMBL322215 1 8.32
CHEMBL607878 1 8.32
CHEMBL2368083 1 7.96
CHEMBL2012670 1 7.92
CHEMBL2368082 1 7.52
CHEMBL129 ZIDOVUDINE 4.0 1 7.42
CHEMBL2368070 1 6.82
CHEMBL2368076 1 6.47
CHEMBL2368078 1 6.21
CHEMBL2368074 1 5.64
CHEMBL2368077 1 5.22
CHEMBL2368081 1 -
CHEMBL2368084 1 -
CHEMBL2368079 1 -
CHEMBL2368073 1 -
CHEMBL2368075 1 -
CHEMBL2368080 1 -
CHEMBL2368071 1 -
CHEMBL607510 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2368072 EC50 = 0.3 nM 9.52
CHEMBL2012671 EC50 = 1.4 nM 8.85
CHEMBL322215 EC50 = 4.8 nM 8.32
CHEMBL607878 EC50 = 4.8 nM 8.32
CHEMBL2368083 EC50 = 11.0 nM 7.96
CHEMBL2012670 EC50 = 12.0 nM 7.92
CHEMBL2368082 EC50 = 30.0 nM 7.52
CHEMBL129 ZIDOVUDINE EC50 = 38.0 nM 7.42
CHEMBL2368070 EC50 = 150.0 nM 6.82
CHEMBL2368076 EC50 = 340.0 nM 6.47
CHEMBL2368078 EC50 = 610.0 nM 6.21
CHEMBL2368074 EC50 = 2300.0 nM 5.64
CHEMBL2368077 EC50 = 6000.0 nM 5.22
CHEMBL2368081 EC50 > 100000.0 nM -
CHEMBL2368084 EC50 = 117000.0 nM -
CHEMBL2368079 EC50 > 100000.0 nM -
CHEMBL2368073 EC50 > 10000.0 nM -
CHEMBL2368075 EC50 > 100000.0 nM -
CHEMBL2368080 EC50 > 100000.0 nM -
CHEMBL2368071 EC50 > 360000.0 nM -
CHEMBL607510 EC50 > 350000.0 nM -