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Assay Detail

CHEMBL4151994

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

Binding
Binding affinity to Texas Red-labelled CXCL12 (unknown origin) assessed as inhibition of CXCL12-Texas Red binding to EGFP-labeled human CXCR4 expressed in HEK293 cell membranes pre-incubated for 1 hr by FRET-based binding assay
ChEMBL ↗
47
Total Activities
47
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Stromal cell-derived factor 1 (CHEMBL3286074) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a Locally and Orally Active CXCL12 Neutraligand (LIT-927) with Anti-inflammatory Effect in a Murine Model of Allergic Airway Hypereosinophilia.
Regenass P, Abboud D, Daubeuf F, Lehalle C, Gizzi P, Riché S, Hachet-Haas M, Rohmer F, Gasparik V, Boeglin D, Haiech J, Knehans T, Rognan D, Heissler D, Marsol C, Villa P, Galzi JL, Hibert M, Frossard N, Bonnet D.
J Med Chem (2018) 61 : 7671 -7686
PubMed 30106292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 47 6.57 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4170392 — — 1 7.60
CHEMBL4160309 — — 1 7.36
CHEMBL4160346 — — 1 7.32
CHEMBL126657 — — 1 7.28
CHEMBL4167574 — — 1 7.28
CHEMBL4175451 — — 1 7.15
CHEMBL4163005 — — 1 6.97
CHEMBL4168923 — — 1 6.97
CHEMBL4169628 — — 1 6.97
CHEMBL4168220 — — 1 6.97
CHEMBL4166275 — — 1 6.97
CHEMBL4160583 — — 1 6.69
CHEMBL4166454 — — 1 6.57
CHEMBL4173832 — — 1 6.54
CHEMBL127593 — — 1 6.46
CHEMBL4162605 — — 1 6.45
CHEMBL4175213 — — 1 6.45
CHEMBL4170951 — — 1 6.45
CHEMBL4169688 — — 1 6.37
CHEMBL4159394 — — 1 6.32
CHEMBL4175047 — — 1 6.30
CHEMBL226710 — — 1 6.20
CHEMBL4164132 — — 1 6.15
CHEMBL4167307 — — 1 5.97
CHEMBL243400 — — 1 5.97
CHEMBL4159676 — — 1 5.86
CHEMBL4163644 — — 1 5.78
CHEMBL130639 — — 1 5.75
CHEMBL4177186 — — 1 5.27
CHEMBL4177375 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4170392 — Ki = 25.0 nM 7.60
CHEMBL4160309 — Ki = 44.0 nM 7.36
CHEMBL4160346 — Ki = 48.0 nM 7.32
CHEMBL126657 — Ki = 53.0 nM 7.28
CHEMBL4167574 — Ki = 53.0 nM 7.28
CHEMBL4175451 — Ki = 71.0 nM 7.15
CHEMBL4166275 — Ki = 107.0 nM 6.97
CHEMBL4168220 — Ki = 107.0 nM 6.97
CHEMBL4163005 — Ki = 107.0 nM 6.97
CHEMBL4169628 — Ki = 107.0 nM 6.97
CHEMBL4168923 — Ki = 107.0 nM 6.97
CHEMBL4160583 — Ki = 203.0 nM 6.69
CHEMBL4166454 — Ki = 267.0 nM 6.57
CHEMBL4173832 — Ki = 285.0 nM 6.54
CHEMBL127593 — Ki = 350.0 nM 6.46
CHEMBL4162605 — Ki = 357.0 nM 6.45
CHEMBL4170951 — Ki = 357.0 nM 6.45
CHEMBL4175213 — Ki = 357.0 nM 6.45
CHEMBL4169688 — Ki = 430.0 nM 6.37
CHEMBL4159394 — Ki = 475.0 nM 6.32
CHEMBL4175047 — Ki = 496.0 nM 6.30
CHEMBL226710 — Ki = 625.0 nM 6.20
CHEMBL4164132 — Ki = 714.0 nM 6.15
CHEMBL4167307 — Ki = 1071.0 nM 5.97
CHEMBL243400 — Ki = 1070.0 nM 5.97
CHEMBL4159676 — Ki = 1380.0 nM 5.86
CHEMBL4163644 — Ki = 1680.0 nM 5.78
CHEMBL130639 — Ki = 1780.0 nM 5.75
CHEMBL4177186 — Ki = 5350.0 nM 5.27
CHEMBL2178112 — Ki > 10000.0 nM -
CHEMBL224637 — Ki > 10000.0 nM -
CHEMBL4173930 — Ki > 10000.0 nM -
CHEMBL376598 — Ki > 10000.0 nM -
CHEMBL227926 — Ki > 10000.0 nM -
CHEMBL4170694 — Ki > 10000.0 nM -
CHEMBL4162758 — Ki > 10000.0 nM -
CHEMBL4174118 — Ki > 5000.0 nM -
CHEMBL4166202 — Ki > 10000.0 nM -
CHEMBL4173759 — Ki > 10000.0 nM -
CHEMBL4160730 — Ki > 10000.0 nM -
CHEMBL4162350 — Ki > 10000.0 nM -
CHEMBL4174763 — Ki > 10000.0 nM -
CHEMBL4164112 — Ki > 10000.0 nM -
CHEMBL4169514 — Ki > 10000.0 nM -
CHEMBL4174364 — Ki > 10000.0 nM -
CHEMBL465025 — Ki > 10000.0 nM -
CHEMBL4177375 — Ki > 10000.0 nM -