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Assay Detail

CHEMBL712397

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

Functional
Concentration required to protect the virus infected cells against viral cytopathicity was measured on HIV-1(IIIB) virus strain in MT-4 cells
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT4
Confidence 1 — Organism
Curated By Expert

Target

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

Publication

Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-tetraazamacrocycles that inhibit HIV replication. Effects of macrocyclic ring size and substituents on the aromatic linker.
Bridger GJ, Skerlj RT, Thornton D, Padmanabhan S, Martellucci SA, Henson GW, Abrams MJ, Yamamoto N, De Vreese K, Pauwels R.
J Med Chem (1995) 38 : 366 -378
PubMed 7830280 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 42 6.79 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2373140 1 8.48
CHEMBL1788331 1 8.38
CHEMBL1788333 1 8.24
CHEMBL1743684 1 8.21
CHEMBL1788349 1 8.19
CHEMBL1788332 1 8.10
CHEMBL122487 1 8.10
CHEMBL1788348 1 7.97
CHEMBL124142 1,1'-[1,4-phenylenebis(methylene)]bis[1,4,8,11-tetraazacyclotetradecane]copper Heptahydrate (7H2O) 1 7.74
CHEMBL1788344 1 7.60
CHEMBL1788330 1 7.47
CHEMBL1788335 1 7.46
CHEMBL1788352 1 7.39
CHEMBL1788338 1 7.39
CHEMBL1743680 1 7.26
CHEMBL1788334 1 7.19
CHEMBL1743683 1 7.12
CHEMBL122048 1 7.07
CHEMBL1788346 1 7.07
CHEMBL1743677 1 6.97
CHEMBL1788347 1 6.86
CHEMBL1743679 1 6.80
CHEMBL1788345 1 6.78
CHEMBL1788339 1 6.69
CHEMBL332659 1 6.50
CHEMBL1743681 1 6.49
CHEMBL1743685 1 6.49
CHEMBL121707 1 6.43
CHEMBL1788350 1 6.39
CHEMBL1788336 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2373140 EC50 = 3.3 nM 8.48
CHEMBL1788331 EC50 = 4.2 nM 8.38
CHEMBL1788333 EC50 = 5.8 nM 8.24
CHEMBL1743684 EC50 = 6.1 nM 8.21
CHEMBL1788349 EC50 = 6.4 nM 8.19
CHEMBL1788332 EC50 = 7.9 nM 8.10
CHEMBL122487 EC50 = 7.9 nM 8.10
CHEMBL1788348 EC50 = 10.7 nM 7.97
CHEMBL124142 1,1'-[1,4-phenylenebis(methylene)]bis[1,4,8,11-tetraazacyclotetradecane]copper Heptahydrate (7H2O) EC50 = 18.1 nM 7.74
CHEMBL1788344 EC50 = 25.3 nM 7.60
CHEMBL1788330 EC50 = 33.7 nM 7.47
CHEMBL1788335 EC50 = 34.7 nM 7.46
CHEMBL1788352 EC50 = 40.8 nM 7.39
CHEMBL1788338 EC50 = 40.6 nM 7.39
CHEMBL1743680 EC50 = 55.0 nM 7.26
CHEMBL1788334 EC50 = 65.0 nM 7.19
CHEMBL1743683 EC50 = 75.1 nM 7.12
CHEMBL122048 EC50 = 84.3 nM 7.07
CHEMBL1788346 EC50 = 84.5 nM 7.07
CHEMBL1743677 EC50 = 106.2 nM 6.97
CHEMBL1788347 EC50 = 138.3 nM 6.86
CHEMBL1743679 EC50 = 157.2 nM 6.80
CHEMBL1788345 EC50 = 166.8 nM 6.78
CHEMBL1788339 EC50 = 206.0 nM 6.69
CHEMBL332659 EC50 = 317.7 nM 6.50
CHEMBL1743681 EC50 = 321.8 nM 6.49
CHEMBL1743685 EC50 = 322.6 nM 6.49
CHEMBL121707 EC50 = 373.0 nM 6.43
CHEMBL1788350 EC50 = 402.5 nM 6.39
CHEMBL1788336 EC50 = 505.9 nM 6.30
CHEMBL1788337 EC50 = 528.7 nM 6.28
CHEMBL1788343 EC50 = 1357.4 nM 5.87
CHEMBL122226 EC50 = 1416.9 nM 5.85
CHEMBL1743682 EC50 = 1671.4 nM 5.78
CHEMBL341527 EC50 = 2433.6 nM 5.61
CHEMBL1788342 EC50 = 2724.7 nM 5.57
CHEMBL1788351 EC50 = 7794.7 nM 5.11
CHEMBL1788341 EC50 = 9130.1 nM 5.04
CHEMBL1743678 EC50 = 14852.0 nM 4.83
CHEMBL1788340 EC50 = 16739.0 nM 4.78
CHEMBL369450 1,1'-[1,4-phenylenebis(methylene)]bis[1,4,8,11-tetraazacyclotetradecane] Palladium Diperchlorate Tetrahydrate (4H2O) EC50 = 31548.0 nM 4.50
CHEMBL125150 EC50 = 399000.0 nM -