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Assay Detail

CHEMBL2215086

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Functional
Allosteric modulation at human CCR8 transfected in COS7 cells 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 8 (CHEMBL4596) ↗
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 5.47 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2205805 — — 2 6.41
CHEMBL99384 — — 2 6.32
CHEMBL593442 — — 2 6.30
CHEMBL316589 — — 2 6.20
CHEMBL2205810 — — 2 6.20
CHEMBL98682 — — 2 5.70
CHEMBL317115 — — 2 5.52
CHEMBL101165 — — 2 5.50
CHEMBL415879 PHENANTHROLINE — 2 5.41
CHEMBL2205806 — — 2 5.32
CHEMBL89445 TERPYRIDINE — 2 5.31
CHEMBL2205808 — — 2 5.30
CHEMBL2205809 — — 2 5.20
CHEMBL2205807 ABAMETAPIR 4.0 2 5.12
CHEMBL2205801 — — 2 4.82
CHEMBL39879 DIPYRIDYL — 2 4.40
CHEMBL1623498 — — 2 4.10
CHEMBL375781 NEOCUPROINE — 2 -
CHEMBL2205802 — — 2 -
CHEMBL2205803 — — 2 -
CHEMBL1976682 — — 2 -
CHEMBL2205804 — — 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2205805 — EC50 = 390.0 nM 6.41
CHEMBL2205805 — EC50 = 398.11 nM 6.40
CHEMBL99384 — EC50 = 480.0 nM 6.32
CHEMBL593442 — EC50 = 501.19 nM 6.30
CHEMBL99384 — EC50 = 501.19 nM 6.30
CHEMBL593442 — EC50 = 520.0 nM 6.28
CHEMBL2205810 — EC50 = 630.96 nM 6.20
CHEMBL316589 — EC50 = 630.96 nM 6.20
CHEMBL316589 — EC50 = 670.0 nM 6.17
CHEMBL2205810 — EC50 = 670.0 nM 6.17
CHEMBL98682 — EC50 = 1995.26 nM 5.70
CHEMBL98682 — EC50 = 2000.0 nM 5.70
CHEMBL317115 — EC50 = 3000.0 nM 5.52
CHEMBL101165 — EC50 = 3162.28 nM 5.50
CHEMBL317115 — EC50 = 3162.28 nM 5.50
CHEMBL101165 — EC50 = 3300.0 nM 5.48
CHEMBL415879 PHENANTHROLINE EC50 = 3900.0 nM 5.41
CHEMBL415879 PHENANTHROLINE EC50 = 3981.07 nM 5.40
CHEMBL2205806 — EC50 = 4800.0 nM 5.32
CHEMBL89445 TERPYRIDINE EC50 = 4900.0 nM 5.31
CHEMBL2205808 — EC50 = 5011.87 nM 5.30
CHEMBL89445 TERPYRIDINE EC50 = 5011.87 nM 5.30
CHEMBL2205806 — EC50 = 5011.87 nM 5.30
CHEMBL2205808 — EC50 = 5400.0 nM 5.27
CHEMBL2205809 — EC50 = 6309.57 nM 5.20
CHEMBL2205809 — EC50 = 7000.0 nM 5.16
CHEMBL2205807 ABAMETAPIR EC50 = 7500.0 nM 5.12
CHEMBL2205807 ABAMETAPIR EC50 = 7943.28 nM 5.10
CHEMBL2205801 — EC50 = 15000.0 nM 4.82
CHEMBL2205801 — EC50 = 15848.93 nM 4.80
CHEMBL39879 DIPYRIDYL EC50 = 39810.72 nM 4.40
CHEMBL39879 DIPYRIDYL EC50 = 42000.0 nM 4.38
CHEMBL1623498 — EC50 = 79432.82 nM 4.10
CHEMBL1623498 — EC50 = 86000.0 nM 4.07
CHEMBL2205802 — EC50 > 1000000.0 nM -
CHEMBL2205803 — EC50 > 1000000.0 nM -
CHEMBL1976682 — EC50 > 1000000.0 nM -
CHEMBL2205804 — EC50 > 1000000.0 nM -
CHEMBL375781 NEOCUPROINE EC50 > 1000000.0 nM -
CHEMBL375781 NEOCUPROINE EC50 < 1000000.0 nM -
CHEMBL2205802 — EC50 < 1000000.0 nM -
CHEMBL2205803 — EC50 < 1000000.0 nM -
CHEMBL1976682 — EC50 < 1000000.0 nM -
CHEMBL2205804 — EC50 < 1000000.0 nM -