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Assay Detail

CHEMBL2215087

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

Functional
Allosteric modulation at human CCR5 transfected in COS7 cells coexpressing chimeric Gqi4myr assessed as [3H]IP3 turnover by liquid scintillation counting analysis
ChEMBL ↗
44
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 5 (CHEMBL274) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Modulation in selectivity and allosteric properties of small-molecule ligands for CC-chemokine receptors.
Thiele S, Malmgaard-Clausen M, Engel-Andreasen J, Steen A, Rummel PC, Nielsen MC, Gloriam DE, Frimurer TM, Ulven T, Rosenkilde MM.
J Med Chem (2012) 55 : 8164 -8177
PubMed 22957890 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 44 5.20 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99384 — — 2 6.00
CHEMBL316589 — — 2 5.75
CHEMBL2205809 — — 2 5.72
CHEMBL2205810 — — 2 5.70
CHEMBL2205807 ABAMETAPIR 4.0 2 5.64
CHEMBL593442 — — 2 5.60
CHEMBL415879 PHENANTHROLINE — 2 5.31
CHEMBL2205801 — — 2 5.00
CHEMBL101165 — — 2 4.96
CHEMBL39879 DIPYRIDYL — 2 4.72
CHEMBL2205808 — — 2 4.70
CHEMBL89445 TERPYRIDINE — 2 4.54
CHEMBL375781 NEOCUPROINE — 2 4.20
CHEMBL98682 — — 2 -
CHEMBL317115 — — 2 -
CHEMBL1623498 — — 2 -
CHEMBL2205802 — — 2 -
CHEMBL2205803 — — 2 -
CHEMBL1976682 — — 2 -
CHEMBL2205806 — — 2 -
CHEMBL2205804 — — 2 -
CHEMBL2205805 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99384 — EC50 = 1000.0 nM 6.00
CHEMBL99384 — EC50 = 1000.0 nM 6.00
CHEMBL316589 — EC50 = 1800.0 nM 5.75
CHEMBL2205809 — EC50 = 1900.0 nM 5.72
CHEMBL316589 — EC50 = 1995.26 nM 5.70
CHEMBL2205810 — EC50 = 1995.26 nM 5.70
CHEMBL2205809 — EC50 = 1995.26 nM 5.70
CHEMBL2205810 — EC50 = 2200.0 nM 5.66
CHEMBL2205807 ABAMETAPIR EC50 = 2300.0 nM 5.64
CHEMBL593442 — EC50 = 2511.89 nM 5.60
CHEMBL2205807 ABAMETAPIR EC50 = 2511.89 nM 5.60
CHEMBL593442 — EC50 = 2600.0 nM 5.58
CHEMBL415879 PHENANTHROLINE EC50 = 4900.0 nM 5.31
CHEMBL415879 PHENANTHROLINE EC50 = 5011.87 nM 5.30
CHEMBL2205801 — EC50 = 10000.0 nM 5.00
CHEMBL2205801 — EC50 = 10000.0 nM 5.00
CHEMBL101165 — EC50 = 11000.0 nM 4.96
CHEMBL101165 — EC50 = 12589.25 nM 4.90
CHEMBL39879 DIPYRIDYL EC50 = 19000.0 nM 4.72
CHEMBL2205808 — EC50 = 19952.62 nM 4.70
CHEMBL39879 DIPYRIDYL EC50 = 19952.62 nM 4.70
CHEMBL2205808 — EC50 = 22000.0 nM 4.66
CHEMBL89445 TERPYRIDINE EC50 = 29000.0 nM 4.54
CHEMBL89445 TERPYRIDINE EC50 = 31622.78 nM 4.50
CHEMBL375781 NEOCUPROINE EC50 = 63095.73 nM 4.20
CHEMBL375781 NEOCUPROINE EC50 = 67000.0 nM 4.17
CHEMBL2205804 — EC50 < 1000000.0 nM -
CHEMBL1976682 — EC50 < 1000000.0 nM -
CHEMBL2205803 — EC50 < 1000000.0 nM -
CHEMBL2205802 — EC50 < 1000000.0 nM -
CHEMBL1623498 — EC50 < 1000000.0 nM -
CHEMBL317115 — EC50 < 1000000.0 nM -
CHEMBL98682 — EC50 < 1000000.0 nM -
CHEMBL2205806 — EC50 < 1000000.0 nM -
CHEMBL2205805 — EC50 < 1000000.0 nM -
CHEMBL2205804 — EC50 > 1000000.0 nM -
CHEMBL1976682 — EC50 > 1000000.0 nM -
CHEMBL2205803 — EC50 > 1000000.0 nM -
CHEMBL2205802 — EC50 > 1000000.0 nM -
CHEMBL1623498 — EC50 > 1000000.0 nM -
CHEMBL317115 — EC50 > 1000000.0 nM -
CHEMBL2205806 — EC50 > 1000000.0 nM -
CHEMBL98682 — EC50 > 1000000.0 nM -
CHEMBL2205805 — EC50 > 1000000.0 nM -