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Assay Detail

CHEMBL3801461

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

Binding
Displacement of [125I]-TARC from human recombinant CCR4 expressed in CHO cell membranes by scintillation counting method
22
Total Activities
22
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
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
Ki 21 7.75 9.00
pKi 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3797662 1 9.00
CHEMBL3799266 1 8.80
CHEMBL372399 1 8.60
CHEMBL3797537 1 8.60
CHEMBL2018954 1 8.50
CHEMBL3799578 1 8.50
CHEMBL3798452 1 8.40
CHEMBL3799393 1 8.30
CHEMBL3799025 1 7.80
CHEMBL3797567 1 7.70
CHEMBL3799865 1 7.60
CHEMBL3799514 1 7.60
CHEMBL3798263 1 7.60
CHEMBL3797980 1 7.60
CHEMBL3798941 1 7.30
CHEMBL3798949 1 7.30
CHEMBL3798539 1 7.00
CHEMBL3799904 1 7.00
CHEMBL3797946 1 6.90
CHEMBL3797678 1 6.50
CHEMBL3797555 1 6.20
CHEMBL3799959 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3797662 Ki = 1.0 nM 9.00
CHEMBL3799266 Ki = 1.585 nM 8.80
CHEMBL372399 Ki = 2.512 nM 8.60
CHEMBL3797537 Ki = 2.512 nM 8.60
CHEMBL2018954 Ki = 3.162 nM 8.50
CHEMBL3799578 Ki = 3.162 nM 8.50
CHEMBL3798452 Ki = 3.981 nM 8.40
CHEMBL3799393 Ki = 5.012 nM 8.30
CHEMBL3799025 Ki = 15.85 nM 7.80
CHEMBL3797567 Ki = 19.95 nM 7.70
CHEMBL3799865 Ki = 25.12 nM 7.60
CHEMBL3799514 Ki = 25.12 nM 7.60
CHEMBL3798263 Ki = 25.12 nM 7.60
CHEMBL3797980 Ki = 25.12 nM 7.60
CHEMBL3798941 Ki = 50.12 nM 7.30
CHEMBL3798949 Ki = 50.12 nM 7.30
CHEMBL3798539 Ki = 100.0 nM 7.00
CHEMBL3799904 Ki = 100.0 nM 7.00
CHEMBL3797946 Ki = 125.89 nM 6.90
CHEMBL3797678 Ki = 316.23 nM 6.50
CHEMBL3797555 Ki = 630.96 nM 6.20
CHEMBL3799959 pKi - -