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Assay Detail

CHEMBL1024326

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

Functional
Antiviral activity against HIV1 expressed in 293T cells assessed as protection against viral M33 envelope infection in human U87 cells coexpressing CD4, CCR5 receptors after 72 hrs by luciferase reporter gene pseudoviral assay
ChEMBL ↗
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type 293T
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378) ↗
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Heterobiaryl human immunodeficiency virus entry inhibitors.
Lu RJ, Tucker JA, Pickens J, Ma YA, Zinevitch T, Kirichenko O, Konoplev V, Kuznetsova S, Sviridov S, Brahmachary E, Khasanov A, Mikel C, Yang Y, Liu C, Wang J, Freel S, Fisher S, Sullivan A, Zhou J, Stanfield-Oakley S, Baker B, Sailstad J, Greenberg M, Bolognesi D, Bray B, Koszalka B, Jeffs P, Jeffries C, Chucholowski A, Sexton C.
J Med Chem (2009) 52 : 4481 -4487
PubMed 19534463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 6.23 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL564185 — — 1 8.15
CHEMBL337301 — — 1 8.10
CHEMBL238103 — — 1 7.58
CHEMBL564694 — — 1 7.46
CHEMBL549542 — — 1 7.34
CHEMBL562433 — — 1 7.30
CHEMBL561027 — — 1 7.25
CHEMBL554934 — — 1 7.11
CHEMBL556253 — — 1 6.96
CHEMBL551638 — — 1 6.89
CHEMBL549537 — — 1 6.80
CHEMBL556252 — — 1 6.60
CHEMBL560834 — — 1 6.60
CHEMBL562553 — — 1 6.50
CHEMBL557888 — — 1 6.48
CHEMBL560096 — — 1 6.38
CHEMBL564340 — — 1 6.36
CHEMBL562429 — — 1 6.27
CHEMBL550279 — — 1 6.20
CHEMBL559568 — — 1 6.08
CHEMBL559440 — — 1 6.06
CHEMBL559823 — — 1 6.04
CHEMBL560694 — — 1 6.03
CHEMBL538684 — — 1 6.00
CHEMBL564047 — — 1 5.96
CHEMBL550684 — — 1 5.92
CHEMBL558875 — — 1 5.92
CHEMBL563167 — — 1 5.85
CHEMBL557276 — — 1 5.80
CHEMBL550217 — — 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL564185 — IC50 = 7.0 nM 8.15
CHEMBL337301 — IC50 = 8.0 nM 8.10
CHEMBL238103 — IC50 = 26.0 nM 7.58
CHEMBL564694 — IC50 = 35.0 nM 7.46
CHEMBL549542 — IC50 = 46.0 nM 7.34
CHEMBL562433 — IC50 = 50.0 nM 7.30
CHEMBL561027 — IC50 = 56.0 nM 7.25
CHEMBL554934 — IC50 = 78.0 nM 7.11
CHEMBL556253 — IC50 = 110.0 nM 6.96
CHEMBL551638 — IC50 = 130.0 nM 6.89
CHEMBL549537 — IC50 = 160.0 nM 6.80
CHEMBL556252 — IC50 = 250.0 nM 6.60
CHEMBL560834 — IC50 = 250.0 nM 6.60
CHEMBL562553 — IC50 = 320.0 nM 6.50
CHEMBL557888 — IC50 = 330.0 nM 6.48
CHEMBL560096 — IC50 = 420.0 nM 6.38
CHEMBL564340 — IC50 = 440.0 nM 6.36
CHEMBL562429 — IC50 = 540.0 nM 6.27
CHEMBL550279 — IC50 = 630.0 nM 6.20
CHEMBL559568 — IC50 = 830.0 nM 6.08
CHEMBL559440 — IC50 = 870.0 nM 6.06
CHEMBL559823 — IC50 = 910.0 nM 6.04
CHEMBL560694 — IC50 = 940.0 nM 6.03
CHEMBL538684 — IC50 = 1000.0 nM 6.00
CHEMBL564047 — IC50 = 1100.0 nM 5.96
CHEMBL550684 — IC50 = 1200.0 nM 5.92
CHEMBL558875 — IC50 = 1200.0 nM 5.92
CHEMBL563167 — IC50 = 1400.0 nM 5.85
CHEMBL557276 — IC50 = 1600.0 nM 5.80
CHEMBL550217 — IC50 = 1800.0 nM 5.75
CHEMBL559641 — IC50 = 2000.0 nM 5.70
CHEMBL554515 — IC50 = 2200.0 nM 5.66
CHEMBL549874 — IC50 = 2500.0 nM 5.60
CHEMBL562865 — IC50 = 2800.0 nM 5.55
CHEMBL562354 — IC50 = 5400.0 nM 5.27
CHEMBL550829 — IC50 = 5400.0 nM 5.27
CHEMBL550830 — IC50 = 6700.0 nM 5.17
CHEMBL561219 — IC50 = 7300.0 nM 5.14
CHEMBL563879 — IC50 = 12000.0 nM 4.92
CHEMBL551432 — IC50 = 13000.0 nM 4.89
CHEMBL562552 — IC50 = 23000.0 nM 4.64
CHEMBL549336 — IC50 < 5.0 nM -
CHEMBL561636 — IC50 > 10000.0 nM -
CHEMBL561022 — IC50 < 5.0 nM -
CHEMBL551898 — IC50 < 5.0 nM -
CHEMBL236995 — IC50 < 5.0 nM -