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Assay Detail

CHEMBL869752

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

Functional
Antagonist activity against human recombinant CXCR4 expressed in CHO cells assessed as inhibition of human SDF1-alpha-stimulated calcium mobilization
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Design, synthesis, and biological evaluation of the combinatorial library with a new spirodiketopiperazine scaffold. Discovery of novel potent and selective low-molecular-weight CCR5 antagonists.
Habashita H, Kokubo M, Hamano S, Hamanaka N, Toda M, Shibayama S, Tada H, Sagawa K, Fukushima D, Maeda K, Mitsuya H.
J Med Chem (2006) 49 : 4140 -4152
PubMed 16821774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.17 5.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL536288 1 5.17
CHEMBL556188 1 -
CHEMBL540108 1 -
CHEMBL556798 1 -
CHEMBL540366 1 -
CHEMBL536743 1 -
CHEMBL537424 1 -
CHEMBL557015 1 -
CHEMBL538084 1 -
CHEMBL537425 1 -
CHEMBL557199 1 -
CHEMBL557150 1 -
CHEMBL535616 1 -
CHEMBL536063 1 -
CHEMBL539854 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL536288 IC50 = 6700.0 nM 5.17
CHEMBL556188 IC50 > 30000.0 nM -
CHEMBL540108 IC50 > 10000.0 nM -
CHEMBL556798 IC50 > 10000.0 nM -
CHEMBL540366 IC50 > 10000.0 nM -
CHEMBL536743 IC50 > 10000.0 nM -
CHEMBL537424 IC50 > 10000.0 nM -
CHEMBL557015 IC50 > 30000.0 nM -
CHEMBL538084 IC50 > 10000.0 nM -
CHEMBL537425 IC50 > 10000.0 nM -
CHEMBL557199 IC50 > 30000.0 nM -
CHEMBL557150 IC50 > 30000.0 nM -
CHEMBL535616 IC50 > 10000.0 nM -
CHEMBL536063 IC50 > 10000.0 nM -
CHEMBL539854 IC50 > 30000.0 nM -