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Assay Detail

CHEMBL3801463

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

Binding
Antagonist activity at CCR4 in human PBMC assessed as inhibition of actin polymerization by flow cytometry
23
Total Activities
23
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
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
pA2 18 - -
Kd 5 6.45 6.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL372399 1 6.76
CHEMBL3799266 1 6.70
CHEMBL2018954 1 6.60
CHEMBL2018969 1 6.20
CHEMBL3797662 1 6.00
CHEMBL3799904 1 -
CHEMBL3797980 1 -
CHEMBL3797567 1 -
CHEMBL3798941 1 -
CHEMBL3798949 1 -
CHEMBL3797946 1 -
CHEMBL3797555 1 -
CHEMBL3798539 1 -
CHEMBL3799025 1 -
CHEMBL3798263 1 -
CHEMBL3798452 1 -
CHEMBL3799393 1 -
CHEMBL3797537 1 -
CHEMBL3799865 1 -
CHEMBL3799578 1 -
CHEMBL3799514 1 -
CHEMBL3797678 1 -
CHEMBL3799959 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL372399 Kd = 173.78 nM 6.76
CHEMBL3799266 Kd = 199.53 nM 6.70
CHEMBL2018954 Kd = 251.19 nM 6.60
CHEMBL2018969 Kd = 630.96 nM 6.20
CHEMBL3797662 Kd = 1000.0 nM 6.00
CHEMBL3799904 pA2 - -
CHEMBL3797980 pA2 - -
CHEMBL3797567 pA2 - -
CHEMBL3798941 pA2 - -
CHEMBL3798949 pA2 - -
CHEMBL3797946 pA2 - -
CHEMBL3797555 pA2 - -
CHEMBL3798539 pA2 - -
CHEMBL3799025 pA2 - -
CHEMBL3798263 pA2 - -
CHEMBL3798452 pA2 - -
CHEMBL3799393 pA2 - -
CHEMBL3797537 pA2 - -
CHEMBL3799865 pA2 - -
CHEMBL3799578 pA2 - -
CHEMBL3799514 pA2 - -
CHEMBL3797678 pA2 - -
CHEMBL3799959 pA2 - -