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Assay Detail

CHEMBL1107998

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

ADMET
Cytotoxicity against human MT4 cells expressing CD4 and CXCR4 assessed as cell viability
38
Total Activities
38
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type MT4
Confidence 1 — Organism
Curated By Autocuration

Target

MT4 (CHEMBL388)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Skerlj RT, Bridger GJ, Kaller A, McEachern EJ, Crawford JB, Zhou Y, Atsma B, Langille J, Nan S, Veale D, Wilson T, Harwig C, Hatse S, Princen K, De Clercq E, Schols D.
J Med Chem (2010) 53 : 3376 -3388
PubMed 20297846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
CC50 37 - -
IC50 1 6.97 6.97

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093149 1 6.97
CHEMBL1092301 1 -
CHEMBL1090513 1 -
CHEMBL1093137 1 -
CHEMBL1089434 1 -
CHEMBL1089100 1 -
CHEMBL1091557 1 -
CHEMBL1091176 1 -
CHEMBL1091175 1 -
CHEMBL1091174 1 -
CHEMBL1088858 1 -
CHEMBL1090514 1 -
CHEMBL1090509 1 -
CHEMBL1092629 1 -
CHEMBL1092628 1 -
CHEMBL1092302 1 -
CHEMBL1088916 1 -
CHEMBL1092596 1 -
CHEMBL1088913 1 -
CHEMBL1088912 1 -
CHEMBL1093302 1 -
CHEMBL1089846 1 -
CHEMBL1089845 1 -
CHEMBL1089844 1 -
CHEMBL1093008 1 -
CHEMBL1088867 1 -
CHEMBL1092324 1 -
CHEMBL1092323 1 -
CHEMBL1092905 1 -
CHEMBL1092322 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093149 IC50 = 108.0 nM 6.97
CHEMBL1093137 CC50 = 380.0 nM -
CHEMBL1090514 CC50 = 44000.0 nM -
CHEMBL1088858 CC50 > 118000.0 nM -
CHEMBL1091174 CC50 = 21000.0 nM -
CHEMBL1091175 CC50 = 500.0 nM -
CHEMBL1091176 CC50 = 126000.0 nM -
CHEMBL1091557 CC50 = 23000.0 nM -
CHEMBL1089100 CC50 = 21000.0 nM -
CHEMBL1089434 CC50 = 23000.0 nM -
CHEMBL1090509 CC50 = 2470.0 nM -
CHEMBL1090513 CC50 = 124000.0 nM -
CHEMBL1090510 CC50 = 21000.0 nM -
CHEMBL1093455 CC50 = 8000.0 nM -
CHEMBL1091201 CC50 = 204000.0 nM -
CHEMBL1089868 CC50 = 22300.0 nM -
CHEMBL1090194 CC50 = 23100.0 nM -
CHEMBL1092252 CC50 = 101000.0 nM -
CHEMBL1092253 CC50 = 37500.0 nM -
CHEMBL1092254 CC50 = 36800.0 nM -
CHEMBL1089846 CC50 = 10800.0 nM -
CHEMBL1092322 CC50 = 34300.0 nM -
CHEMBL1092905 CC50 = 26400.0 nM -
CHEMBL1092323 CC50 = 126800.0 nM -
CHEMBL1092324 CC50 = 238000.0 nM -
CHEMBL1088867 CC50 = 45900.0 nM -
CHEMBL1093008 CC50 = 29600.0 nM -
CHEMBL1089844 CC50 = 51900.0 nM -
CHEMBL1089845 CC50 = 50800.0 nM -
CHEMBL1092629 CC50 = 152000.0 nM -
CHEMBL1093302 CC50 = 6860.0 nM -
CHEMBL1088912 CC50 = 32900.0 nM -
CHEMBL1088913 CC50 = 160000.0 nM -
CHEMBL1092596 CC50 = 30200.0 nM -
CHEMBL1088916 CC50 = 30200.0 nM -
CHEMBL1092301 CC50 = 29500.0 nM -
CHEMBL1092302 CC50 = 28200.0 nM -
CHEMBL1092628 CC50 = 55300.0 nM -