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Assay Detail

CHEMBL944771

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

Binding
Inhibition of HIV NL43 recombinant reverse transcriptase K103N mutant by scintillation proximity assay
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus
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

Novel indole-3-sulfonamides as potent HIV non-nucleoside reverse transcriptase inhibitors (NNRTIs).
Zhao Z, Wolkenberg SE, Sanderson PE, Lu M, Munshi V, Moyer G, Feng M, Carella AV, Ecto LT, Gabryelski LJ, Lai MT, Prasad SG, Yan Y, McGaughey GB, Miller MD, Lindsley CW, Hartman GD, Vacca JP, Williams TM.
Bioorg Med Chem Lett (2008) 18 : 554 -559
PubMed 18083561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.69 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL253018 1 8.05
CHEMBL252405 1 7.70
CHEMBL403784 1 7.60
CHEMBL252406 1 7.51
CHEMBL252608 1 7.38
CHEMBL400045 1 7.32
CHEMBL252609 1 7.21
CHEMBL252607 1 7.03
CHEMBL252810 1 6.96
CHEMBL283950 L-737126 1 6.94
CHEMBL253016 1 6.82
CHEMBL252811 1 6.82
CHEMBL252603 1 6.77
CHEMBL253017 1 6.66
CHEMBL252407 1 6.58
CHEMBL403783 1 6.55
CHEMBL252812 1 6.55
CHEMBL398419 1 6.43
CHEMBL403126 1 5.71
CHEMBL252795 1 5.64
CHEMBL264320 1 5.55
CHEMBL401342 1 5.09
CHEMBL253629 1 5.00
CHEMBL252805 1 -
CHEMBL443318 1 -
CHEMBL400903 1 -
CHEMBL253638 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL253018 IC50 = 9.0 nM 8.05
CHEMBL252405 IC50 = 20.0 nM 7.70
CHEMBL403784 IC50 = 25.0 nM 7.60
CHEMBL252406 IC50 = 31.0 nM 7.51
CHEMBL252608 IC50 = 42.0 nM 7.38
CHEMBL400045 IC50 = 48.0 nM 7.32
CHEMBL252609 IC50 = 62.0 nM 7.21
CHEMBL252607 IC50 = 93.0 nM 7.03
CHEMBL252810 IC50 = 110.0 nM 6.96
CHEMBL283950 L-737126 IC50 = 116.0 nM 6.94
CHEMBL253016 IC50 = 150.0 nM 6.82
CHEMBL252811 IC50 = 150.0 nM 6.82
CHEMBL252603 IC50 = 170.0 nM 6.77
CHEMBL253017 IC50 = 220.0 nM 6.66
CHEMBL252407 IC50 = 260.0 nM 6.58
CHEMBL403783 IC50 = 280.0 nM 6.55
CHEMBL252812 IC50 = 280.0 nM 6.55
CHEMBL398419 IC50 = 370.0 nM 6.43
CHEMBL403126 IC50 = 1963.0 nM 5.71
CHEMBL252795 IC50 = 2300.0 nM 5.64
CHEMBL264320 IC50 = 2800.0 nM 5.55
CHEMBL401342 IC50 = 8200.0 nM 5.09
CHEMBL253629 IC50 = 10000.0 nM 5.00
CHEMBL252805 IC50 - -
CHEMBL443318 IC50 - -
CHEMBL400903 IC50 - -
CHEMBL253638 IC50 - -