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Assay Detail

CHEMBL802769

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

Binding
Inhibition of HIV-1 Reverse transcriptase using poly-(rc)-oligo(dg) as the template primer.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Novel modifications in the alkenyldiarylmethane (ADAM) series of non-nucleoside reverse transcriptase inhibitors.
Casimiro-Garcia A, Micklatcher M, Turpin JA, Stup TL, Watson K, Buckheit RW, Cushman M.
J Med Chem (1999) 42 : 4861 -4874
PubMed 10579849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.41 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294840 1 6.52
CHEMBL107200 1 6.52
CHEMBL144701 1 6.33
CHEMBL141323 1 6.00
CHEMBL357187 1 5.89
CHEMBL343149 1 5.66
CHEMBL144209 1 5.50
CHEMBL357658 1 5.50
CHEMBL145842 1 5.50
CHEMBL343398 1 5.31
CHEMBL142532 1 5.14
CHEMBL131432 1 5.00
CHEMBL144654 1 4.96
CHEMBL144509 1 4.50
CHEMBL144121 1 4.16
CHEMBL359242 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294840 IC50 = 300.0 nM 6.52
CHEMBL107200 IC50 = 300.0 nM 6.52
CHEMBL144701 IC50 = 470.0 nM 6.33
CHEMBL141323 IC50 = 1000.0 nM 6.00
CHEMBL357187 IC50 = 1300.0 nM 5.89
CHEMBL343149 IC50 = 2200.0 nM 5.66
CHEMBL144209 IC50 = 3200.0 nM 5.50
CHEMBL357658 IC50 = 3200.0 nM 5.50
CHEMBL145842 IC50 = 3200.0 nM 5.50
CHEMBL343398 IC50 = 4900.0 nM 5.31
CHEMBL142532 IC50 = 7200.0 nM 5.14
CHEMBL131432 IC50 = 10000.0 nM 5.00
CHEMBL144654 IC50 = 11000.0 nM 4.96
CHEMBL144509 IC50 = 31600.0 nM 4.50
CHEMBL144121 IC50 = 70000.0 nM 4.16
CHEMBL359242 IC50 = 100000.0 nM 4.00