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Assay Detail

CHEMBL712344

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

Functional
Effective concentration for 50% protection of HIV-induced cytopathogenicity in MT-4 cells on the MTT assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type MT4
Confidence 8 — Homologous single protein target
Curated By Expert

Target

C-X-C chemokine receptor type 4 (CHEMBL2107)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of specific CXCR4 inhibitors possessing high selectivity indexes as well as complete stability in serum based on an anti-HIV peptide T140.
Tamamura H, Omagari A, Hiramatsu K, Gotoh K, Kanamoto T, Xu Y, Kodama E, Matsuoka M, Hattori T, Yamamoto N, Nakashima H, Otaka A, Fujii N.
Bioorg Med Chem Lett (2001) 11 : 1897 -1902
PubMed 11459656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 8.18 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2372985 1 9.40
CHEMBL2372997 1 9.30
CHEMBL2372993 1 9.22
CHEMBL2373004 1 8.92
CHEMBL2372989 1 8.57
CHEMBL2373002 1 8.55
CHEMBL2372983 1 8.48
CHEMBL2372994 1 8.40
CHEMBL2373001 1 8.34
CHEMBL2372999 1 8.18
CHEMBL2372995 1 8.17
CHEMBL2372990 1 8.11
CHEMBL2372996 1 8.05
CHEMBL2373005 1 7.44
CHEMBL2373000 1 7.43
CHEMBL2373003 1 7.40
CHEMBL2372986 1 7.17
CHEMBL2372998 1 7.14
CHEMBL853 ZALCITABINE 4.0 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2372985 EC50 = 0.4 nM 9.40
CHEMBL2372997 EC50 = 0.5 nM 9.30
CHEMBL2372993 EC50 = 0.6 nM 9.22
CHEMBL2373004 EC50 = 1.2 nM 8.92
CHEMBL2372989 EC50 = 2.7 nM 8.57
CHEMBL2373002 EC50 = 2.8 nM 8.55
CHEMBL2372983 EC50 = 3.3 nM 8.48
CHEMBL2372994 EC50 = 4.0 nM 8.40
CHEMBL2373001 EC50 = 4.6 nM 8.34
CHEMBL2372999 EC50 = 6.6 nM 8.18
CHEMBL2372995 EC50 = 6.8 nM 8.17
CHEMBL2372990 EC50 = 7.8 nM 8.11
CHEMBL2372996 EC50 = 8.9 nM 8.05
CHEMBL2373005 EC50 = 36.0 nM 7.44
CHEMBL2373000 EC50 = 37.0 nM 7.43
CHEMBL2373003 EC50 = 40.0 nM 7.40
CHEMBL2372986 EC50 = 68.0 nM 7.17
CHEMBL2372998 EC50 = 72.0 nM 7.14
CHEMBL853 ZALCITABINE EC50 = 88.0 nM 7.06