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Assay Detail

CHEMBL712403

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

Functional
Effective concentration against HIV-2(ROD) replication in MT-4 cells
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 2
Cell Type MT4
Confidence 1 — Organism
Curated By Expert

Target

Human immunodeficiency virus 2 (CHEMBL380)
Type ORGANISM
Organism Human immunodeficiency virus 2

Publication

Synthesis and structure-activity relationships of phenylenebis(methylene)-linked bis-tetraazamacrocycles that inhibit human immunodeficiency virus replication. 2. Effect of heteroaromatic linkers on the activity of bicyclams.
Bridger GJ, Skerlj RT, Padmanabhan S, Martellucci SA, Henson GW, Abrams MJ, Joao HC, Witvrouw M, De Vreese K, Pauwels R, De Clercq E.
J Med Chem (1996) 39 : 109 -119
PubMed 8568797 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 6.90 8.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18442 PLERIXAFOR 4.0 1 8.23
CHEMBL1202144 1 7.76
CHEMBL1202143 1 7.70
CHEMBL275434 1 7.61
CHEMBL277151 1 7.41
CHEMBL17211 1 7.38
CHEMBL1204109 1 7.18
CHEMBL1204110 1 7.15
CHEMBL278202 1 7.11
CHEMBL417454 1 7.03
CHEMBL18628 1 6.23
CHEMBL1202145 1 5.66
CHEMBL18154 1 5.37
CHEMBL1202142 1 4.79
CHEMBL18097 1 -
CHEMBL1202423 1 -
CHEMBL17589 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18442 PLERIXAFOR EC50 = 5.9 nM 8.23
CHEMBL1202144 EC50 = 17.4 nM 7.76
CHEMBL1202143 EC50 = 20.0 nM 7.70
CHEMBL275434 EC50 = 24.6 nM 7.61
CHEMBL277151 EC50 = 39.0 nM 7.41
CHEMBL17211 EC50 = 42.2 nM 7.38
CHEMBL1204109 EC50 = 65.4 nM 7.18
CHEMBL1204110 EC50 = 71.0 nM 7.15
CHEMBL278202 EC50 = 78.6 nM 7.11
CHEMBL417454 EC50 = 93.4 nM 7.03
CHEMBL18628 EC50 = 590.4 nM 6.23
CHEMBL1202145 EC50 = 2194.7 nM 5.66
CHEMBL18154 EC50 = 4274.4 nM 5.37
CHEMBL1202142 EC50 = 16367.0 nM 4.79
CHEMBL18097 EC50 = 203000.0 nM -
CHEMBL1202423 EC50 = 105880.0 nM -
CHEMBL17589 EC50 = 200300.0 nM -