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Assay Detail

CHEMBL1666330

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

Binding
Inhibition of Mab 12G5 binding to CXCR4 W283A mutant expressed in HEK293 cells
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

The novel CXCR4 antagonist KRH-3955 is an orally bioavailable and extremely potent inhibitor of human immunodeficiency virus type 1 infection: comparative studies with AMD3100.
Murakami T, Kumakura S, Yamazaki T, Tanaka R, Hamatake M, Okuma K, Huang W, Toma J, Komano J, Yanaka M, Tanaka Y, Yamamoto N.
Antimicrob Agents Chemother (2009) 53 : 2940 -2948
PubMed 19451305 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 7.71 8.89
IC90 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2062277 2 8.89
CHEMBL18442 PLERIXAFOR 4.0 2 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2062277 IC50 = 1.3 nM 8.89
CHEMBL18442 PLERIXAFOR IC50 = 300.2 nM 6.52
CHEMBL2062277 IC90 = 6.9 nM -
CHEMBL18442 PLERIXAFOR IC90 > 1000.0 nM -