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Assay Detail

CHEMBL654035

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Functional
Antagonistic activity against human C-C chemokine receptor type 5.
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Orally bioavailable competitive CCR5 antagonists.
Thoma G, Nuninger F, Schaefer M, Akyel KG, Albert R, Beerli C, Bruns C, Francotte E, Luyten M, MacKenzie D, Oberer L, Streiff MB, Wagner T, Walter H, Weckbecker G, Zerwes HG.
J Med Chem (2004) 47 : 1939 -1955
PubMed 15055994 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 37 8.02 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59511 1 9.22
CHEMBL58897 1 9.10
CHEMBL61424 1 9.00
CHEMBL301454 1 8.85
CHEMBL61536 1 8.70
CHEMBL292625 1 8.66
CHEMBL58387 1 8.64
CHEMBL60225 1 8.64
CHEMBL58441 1 8.62
CHEMBL61466 1 8.62
CHEMBL62152 1 8.59
CHEMBL61373 1 8.55
CHEMBL58004 1 8.54
CHEMBL61828 1 8.52
CHEMBL556314 1 8.48
CHEMBL59328 1 8.43
CHEMBL58248 1 8.42
CHEMBL59101 1 8.11
CHEMBL59602 1 8.09
CHEMBL61374 1 8.07
CHEMBL58109 1 8.05
CHEMBL293900 1 8.00
CHEMBL58101 1 7.96
CHEMBL60589 1 7.39
CHEMBL58176 1 7.38
CHEMBL60711 1 7.32
CHEMBL416512 1 7.12
CHEMBL418120 1 7.10
CHEMBL60279 1 7.04
CHEMBL61465 1 7.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59511 IC50 = 0.6 nM 9.22
CHEMBL58897 IC50 = 0.8 nM 9.10
CHEMBL61424 IC50 = 1.0 nM 9.00
CHEMBL301454 IC50 = 1.4 nM 8.85
CHEMBL61536 IC50 = 2.0 nM 8.70
CHEMBL292625 IC50 = 2.2 nM 8.66
CHEMBL58387 IC50 = 2.3 nM 8.64
CHEMBL60225 IC50 = 2.3 nM 8.64
CHEMBL58441 IC50 = 2.4 nM 8.62
CHEMBL61466 IC50 = 2.4 nM 8.62
CHEMBL62152 IC50 = 2.6 nM 8.59
CHEMBL61373 IC50 = 2.8 nM 8.55
CHEMBL58004 IC50 = 2.9 nM 8.54
CHEMBL61828 IC50 = 3.0 nM 8.52
CHEMBL556314 IC50 = 3.3 nM 8.48
CHEMBL59328 IC50 = 3.7 nM 8.43
CHEMBL58248 IC50 = 3.8 nM 8.42
CHEMBL59101 IC50 = 7.8 nM 8.11
CHEMBL59602 IC50 = 8.2 nM 8.09
CHEMBL61374 IC50 = 8.5 nM 8.07
CHEMBL58109 IC50 = 9.0 nM 8.05
CHEMBL293900 IC50 = 9.9 nM 8.00
CHEMBL58101 IC50 = 11.1 nM 7.96
CHEMBL60589 IC50 = 41.0 nM 7.39
CHEMBL58176 IC50 = 42.0 nM 7.38
CHEMBL60711 IC50 = 48.0 nM 7.32
CHEMBL416512 IC50 = 75.0 nM 7.12
CHEMBL418120 IC50 = 80.0 nM 7.10
CHEMBL60279 IC50 = 91.0 nM 7.04
CHEMBL61465 IC50 = 100.0 nM 7.00
CHEMBL294271 IC50 = 102.0 nM 6.99
CHEMBL292894 IC50 = 200.0 nM 6.70
CHEMBL433635 IC50 = 408.0 nM 6.39
CHEMBL59285 IC50 = 460.0 nM 6.34
CHEMBL304931 IC50 > 100.0 nM -
CHEMBL59358 IC50 > 1000.0 nM -
CHEMBL59492 IC50 > 1000.0 nM -