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Assay Detail

CHEMBL804265

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

Binding
Inhibition of HIV-1 reverse transcriptase using a poly(rC):oligo(dG)12-18 template primer
9
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structural analogues of the calanolide anti-HIV agents. Modification of the trans-10,11-dimethyldihydropyran-12-ol ring (ring C).
Zembower DE, Liao S, Flavin MT, Xu ZQ, Stup TL, Buckheit RW, Khilevich A, Mar AA, Sheinkman AK.
J Med Chem (1997) 40 : 1005 -1017
PubMed 9083491 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 5.28 6.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267447 CALANOLIDE A 1.0 2 6.50
CHEMBL267693 1 5.70
CHEMBL7840 1 5.50
CHEMBL266552 1 5.30
CHEMBL267679 1 4.50
CHEMBL269090 1 4.40
CHEMBL266091 1 4.30
CHEMBL7378 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267447 CALANOLIDE A EC50 = 320.0 nM 6.50
CHEMBL267447 CALANOLIDE A EC50 = 970.0 nM 6.01
CHEMBL267693 EC50 = 2000.0 nM 5.70
CHEMBL7840 EC50 = 3200.0 nM 5.50
CHEMBL266552 EC50 = 5000.0 nM 5.30
CHEMBL267679 EC50 = 32000.0 nM 4.50
CHEMBL269090 EC50 = 40000.0 nM 4.40
CHEMBL266091 EC50 = 50000.0 nM 4.30
CHEMBL7378 EC50 > 100000.0 nM -