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Assay Detail

CHEMBL3801465

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

Functional
Induction of CCR4 internalisation in human HUT78 cells after 30 mins by flow cytometry
10
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HuT78
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 4 (CHEMBL2414)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,8-Diazaspiro[4.5]decan-8-yl)pyrimidin-4-amine potent CCR4 antagonists capable of inducing receptor endocytosis.
Shukla L, Ajram LA, Begg M, Evans B, Graves RH, Hodgson ST, Lynn SM, Miah AH, Percy JM, Procopiou PA, Richards SA, Slack RJ.
Eur J Med Chem (2016) 115 : 14 -25
PubMed 26991939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.52 8.20
Activity 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3799393 2 8.20
CHEMBL2018953 1 8.00
CHEMBL3798452 2 7.90
CHEMBL3799578 2 7.80
CHEMBL3797662 2 6.80
CHEMBL3797462 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3799393 EC50 = 6.31 nM 8.20
CHEMBL2018953 EC50 = 10.0 nM 8.00
CHEMBL3798452 EC50 = 12.59 nM 7.90
CHEMBL3799578 EC50 = 15.85 nM 7.80
CHEMBL3797662 EC50 = 158.49 nM 6.80
CHEMBL3797462 EC50 = 398.11 nM 6.40
CHEMBL3798452 Activity = 56.0 % -
CHEMBL3799393 Activity = 64.0 % -
CHEMBL3799578 Activity = 62.0 % -
CHEMBL3797662 Activity = 74.0 % -