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Assay Detail

CHEMBL1038041

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

Functional
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus replication after 4 days by MTT assay
29
Total Activities
29
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 Autocuration

Target

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

Publication

Synthesis and structure-activity relationships of azamacrocyclic C-X-C chemokine receptor 4 antagonists: analogues containing a single azamacrocyclic ring are potent inhibitors of T-cell tropic (X4) HIV-1 replication.
Bridger GJ, Skerlj RT, Hernandez-Abad PE, Bogucki DE, Wang Z, Zhou Y, Nan S, Boehringer EM, Wilson T, Crawford J, Metz M, Hatse S, Princen K, De Clercq E, Schols D.
J Med Chem (2010) 53 : 1250 -1260
PubMed 20043638 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 6.33 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL18442 PLERIXAFOR 4.0 1 8.40
CHEMBL585013 1 8.40
CHEMBL477121 1 8.05
CHEMBL565514 1 8.00
CHEMBL569254 1 7.89
CHEMBL569989 1 7.40
CHEMBL566386 1 7.37
CHEMBL569489 1 7.20
CHEMBL569990 1 6.98
CHEMBL565319 1 6.66
CHEMBL565318 1 6.38
CHEMBL569991 1 6.37
CHEMBL569289 1 6.31
CHEMBL478168 1 6.31
CHEMBL565512 1 6.14
CHEMBL583243 1 6.04
CHEMBL569318 1 5.91
CHEMBL584756 1 5.91
CHEMBL567013 1 5.74
CHEMBL569253 1 5.72
CHEMBL568867 1 5.66
CHEMBL584283 1 5.34
CHEMBL583834 1 5.07
CHEMBL567238 1 5.00
CHEMBL578392 1 4.95
CHEMBL583861 1 4.92
CHEMBL567044 1 4.85
CHEMBL565326 1 4.31
CHEMBL577951 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL18442 PLERIXAFOR EC50 = 4.0 nM 8.40
CHEMBL585013 EC50 = 4.0 nM 8.40
CHEMBL477121 EC50 = 9.0 nM 8.05
CHEMBL565514 EC50 = 10.0 nM 8.00
CHEMBL569254 EC50 = 13.0 nM 7.89
CHEMBL569989 EC50 = 40.0 nM 7.40
CHEMBL566386 EC50 = 43.0 nM 7.37
CHEMBL569489 EC50 = 63.0 nM 7.20
CHEMBL569990 EC50 = 104.0 nM 6.98
CHEMBL565319 EC50 = 217.0 nM 6.66
CHEMBL565318 EC50 = 416.0 nM 6.38
CHEMBL569991 EC50 = 426.0 nM 6.37
CHEMBL569289 EC50 = 485.0 nM 6.31
CHEMBL478168 EC50 = 491.0 nM 6.31
CHEMBL565512 EC50 = 717.0 nM 6.14
CHEMBL583243 EC50 = 920.0 nM 6.04
CHEMBL569318 EC50 = 1239.0 nM 5.91
CHEMBL584756 EC50 = 1245.0 nM 5.91
CHEMBL567013 EC50 = 1825.0 nM 5.74
CHEMBL569253 EC50 = 1895.0 nM 5.72
CHEMBL568867 EC50 = 2185.0 nM 5.66
CHEMBL584283 EC50 = 4561.0 nM 5.34
CHEMBL583834 EC50 = 8470.0 nM 5.07
CHEMBL567238 EC50 = 9977.0 nM 5.00
CHEMBL578392 EC50 = 11131.0 nM 4.95
CHEMBL583861 EC50 = 11878.0 nM 4.92
CHEMBL567044 EC50 = 14106.0 nM 4.85
CHEMBL565326 EC50 = 49135.0 nM 4.31
CHEMBL577951 EC50 = 126401.0 nM -