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Assay Detail

CHEMBL832790

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

Binding
Displacement of [125I]-MIP-1 alpha from human C-C chemokine receptor type 5 expressed on CHO cell membranes
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Potent 1,3,4-trisubstituted pyrrolidine CCR5 receptor antagonists: effects of fused heterocycles on antiviral activity and pharmacokinetic properties.
Kim D, Wang L, Hale JJ, Lynch CL, Budhu RJ, Maccoss M, Mills SG, Malkowitz L, Gould SL, DeMartino JA, Springer MS, Hazuda D, Miller M, Kessler J, Hrin RC, Carver G, Carella A, Henry K, Lineberger J, Schleif WA, Emini EA.
Bioorg Med Chem Lett (2005) 15 : 2129 -2134
PubMed 15808483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 8.43 10.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL20896 1 10.00
CHEMBL194497 1 9.52
CHEMBL193984 1 9.46
CHEMBL2113086 1 9.38
CHEMBL371177 1 9.30
CHEMBL195753 1 9.22
CHEMBL193822 1 9.10
CHEMBL435886 1 9.09
CHEMBL193440 1 9.08
CHEMBL193988 1 9.05
CHEMBL2113088 1 9.00
CHEMBL364070 1 8.60
CHEMBL193972 1 8.59
CHEMBL436290 1 8.55
CHEMBL475606 1 8.52
CHEMBL472798 1 8.46
CHEMBL191139 1 8.20
CHEMBL2113084 1 8.15
CHEMBL196087 1 8.09
CHEMBL445925 1 8.00
CHEMBL191803 1 7.92
CHEMBL194078 1 7.92
CHEMBL470512 1 7.89
CHEMBL195930 1 7.64
CHEMBL472799 1 7.54
CHEMBL195199 1 7.20
CHEMBL475777 1 7.19
CHEMBL192456 1 7.00
CHEMBL363564 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL20896 IC50 = 0.1 nM 10.00
CHEMBL194497 IC50 = 0.3 nM 9.52
CHEMBL193984 IC50 = 0.35 nM 9.46
CHEMBL2113086 IC50 = 0.42 nM 9.38
CHEMBL371177 IC50 = 0.5 nM 9.30
CHEMBL195753 IC50 = 0.6 nM 9.22
CHEMBL193822 IC50 = 0.8 nM 9.10
CHEMBL435886 IC50 = 0.82 nM 9.09
CHEMBL193440 IC50 = 0.84 nM 9.08
CHEMBL193988 IC50 = 0.89 nM 9.05
CHEMBL2113088 IC50 = 1.0 nM 9.00
CHEMBL364070 IC50 = 2.5 nM 8.60
CHEMBL193972 IC50 = 2.6 nM 8.59
CHEMBL436290 IC50 = 2.8 nM 8.55
CHEMBL475606 IC50 = 3.0 nM 8.52
CHEMBL472798 IC50 = 3.5 nM 8.46
CHEMBL191139 IC50 = 6.3 nM 8.20
CHEMBL2113084 IC50 = 7.0 nM 8.15
CHEMBL196087 IC50 = 8.2 nM 8.09
CHEMBL445925 IC50 = 10.0 nM 8.00
CHEMBL191803 IC50 = 12.0 nM 7.92
CHEMBL194078 IC50 = 12.0 nM 7.92
CHEMBL470512 IC50 = 13.0 nM 7.89
CHEMBL195930 IC50 = 23.0 nM 7.64
CHEMBL472799 IC50 = 29.0 nM 7.54
CHEMBL195199 IC50 = 63.0 nM 7.20
CHEMBL475777 IC50 = 65.0 nM 7.19
CHEMBL192456 IC50 = 100.0 nM 7.00
CHEMBL363564 IC50 = 200.0 nM 6.70