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Assay Detail

CHEMBL5238907

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

Functional
Antiviral activity against wild type HIV-1 NLRepRlucP373S infected in human MT2 cells assessed as inhibition of viral growth measured after 4 to 5 days in presence of 10% FBS and 40% human serum supplemented with 27 mg/mL of human serum albumin by Dual luciferase reporter assay
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT2
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Synthesis, Structure-Activity Relationships, and <i>In Vivo</i> Evaluation of Novel C-17 Amine Derivatives Based on GSK3640254 as HIV-1 Maturation Inhibitors with Broad Spectrum Activity.
Hartz RA, Xu L, Sit SY, Chen J, Venables BL, Lin Z, Zhang S, Li Z, Parker D, Simmons TS, Jenkins S, Hanumegowda UM, Dicker I, Krystal M, Meanwell NA, Regueiro-Ren A.
J Med Chem (2022) 65 : 15935 -15966
PubMed 36441509 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 26 7.46 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5277711 1 8.23
CHEMBL5201510 FIPRAVIRIMAT 2.0 2 8.18
CHEMBL5285267 1 8.03
CHEMBL3827379 BMS-955176 2.0 1 8.00
CHEMBL5268258 1 7.89
CHEMBL5282269 1 7.85
CHEMBL5270022 1 7.80
CHEMBL5272708 1 7.77
CHEMBL5276163 1 7.75
CHEMBL5276342 1 7.72
CHEMBL5271451 1 7.72
CHEMBL5287720 1 7.72
CHEMBL5280223 1 7.62
CHEMBL5281869 1 7.58
CHEMBL5280411 1 7.57
CHEMBL5273401 1 7.52
CHEMBL5286848 1 7.52
CHEMBL5275924 1 7.44
CHEMBL5288711 1 7.28
CHEMBL5274769 1 7.27
CHEMBL5267277 1 7.08
CHEMBL5287512 1 6.83
CHEMBL5269871 1 6.01
CHEMBL404519 BEVIRIMAT 2.0 1 6.01
CHEMBL5271405 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5277711 EC50 = 5.9 nM 8.23
CHEMBL5201510 FIPRAVIRIMAT EC50 = 6.6 nM 8.18
CHEMBL5285267 EC50 = 9.3 nM 8.03
CHEMBL3827379 BMS-955176 EC50 = 10.0 nM 8.00
CHEMBL5268258 EC50 = 13.0 nM 7.89
CHEMBL5282269 EC50 = 14.0 nM 7.85
CHEMBL5201510 FIPRAVIRIMAT EC50 = 14.0 nM 7.85
CHEMBL5270022 EC50 = 16.0 nM 7.80
CHEMBL5272708 EC50 = 17.0 nM 7.77
CHEMBL5276163 EC50 = 18.0 nM 7.75
CHEMBL5276342 EC50 = 19.0 nM 7.72
CHEMBL5287720 EC50 = 19.0 nM 7.72
CHEMBL5271451 EC50 = 19.0 nM 7.72
CHEMBL5280223 EC50 = 24.0 nM 7.62
CHEMBL5281869 EC50 = 26.0 nM 7.58
CHEMBL5280411 EC50 = 27.0 nM 7.57
CHEMBL5286848 EC50 = 30.0 nM 7.52
CHEMBL5273401 EC50 = 30.0 nM 7.52
CHEMBL5275924 EC50 = 36.0 nM 7.44
CHEMBL5288711 EC50 = 53.0 nM 7.28
CHEMBL5274769 EC50 = 54.0 nM 7.27
CHEMBL5267277 EC50 = 84.0 nM 7.08
CHEMBL5287512 EC50 = 147.0 nM 6.83
CHEMBL5269871 EC50 = 980.0 nM 6.01
CHEMBL404519 BEVIRIMAT EC50 = 970.0 nM 6.01
CHEMBL5271405 EC50 = 1760.0 nM 5.75