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Assay Detail

CHEMBL945751

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

Binding
Displacement of [125I] eotaxin from human CCR3 receptor in CHO cells
38
Total Activities
37
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 Intermediate

Target

C-C chemokine receptor type 3 (CHEMBL3473)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

From rigid cyclic templates to conformationally stabilized acyclic scaffolds. Part II: Acyclic replacements for the (3S)-3-benzylpiperidine in a series of potent CCR3 antagonists.
Gardner DS, Santella JB, Tebben AJ, Batt DG, Ko SS, Traeger SC, Welch PK, Wadman EA, Davies P, Carter PH, Duncia JV.
Bioorg Med Chem Lett (2008) 18 : 586 -595
PubMed 18160284 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 8.57 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL254095 1 9.70
CHEMBL398548 1 9.70
CHEMBL251837 1 9.70
CHEMBL399495 1 9.52
CHEMBL252035 1 9.52
CHEMBL437396 1 9.52
CHEMBL252631 1 9.40
CHEMBL428062 2 9.40
CHEMBL400378 1 9.40
CHEMBL251838 1 9.40
CHEMBL254503 1 9.40
CHEMBL254676 1 9.30
CHEMBL251822 1 9.30
CHEMBL253210 1 9.22
CHEMBL254881 1 9.22
CHEMBL254677 1 9.22
CHEMBL363840 1 9.00
CHEMBL253244 1 8.92
CHEMBL254930 1 8.74
CHEMBL252792 1 8.60
CHEMBL254093 1 8.60
CHEMBL251839 1 8.60
CHEMBL254470 1 8.49
CHEMBL400467 1 8.47
CHEMBL253209 1 8.43
CHEMBL252222 1 8.24
CHEMBL401002 1 8.22
CHEMBL254471 1 8.05
CHEMBL253034 1 7.72
CHEMBL254055 1 7.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL398548 IC50 = 0.2 nM 9.70
CHEMBL251837 IC50 = 0.2 nM 9.70
CHEMBL254095 IC50 = 0.2 nM 9.70
CHEMBL399495 IC50 = 0.3 nM 9.52
CHEMBL252035 IC50 = 0.3 nM 9.52
CHEMBL437396 IC50 = 0.3 nM 9.52
CHEMBL428062 IC50 = 0.4 nM 9.40
CHEMBL254503 IC50 = 0.4 nM 9.40
CHEMBL251838 IC50 = 0.4 nM 9.40
CHEMBL400378 IC50 = 0.4 nM 9.40
CHEMBL428062 IC50 = 0.4 nM 9.40
CHEMBL252631 IC50 = 0.4 nM 9.40
CHEMBL251822 IC50 = 0.5 nM 9.30
CHEMBL254676 IC50 = 0.5 nM 9.30
CHEMBL253210 IC50 = 0.6 nM 9.22
CHEMBL254677 IC50 = 0.6 nM 9.22
CHEMBL254881 IC50 = 0.6 nM 9.22
CHEMBL363840 IC50 = 1.0 nM 9.00
CHEMBL253244 IC50 = 1.2 nM 8.92
CHEMBL254930 IC50 = 1.8 nM 8.74
CHEMBL251839 IC50 = 2.5 nM 8.60
CHEMBL252792 IC50 = 2.5 nM 8.60
CHEMBL254093 IC50 = 2.5 nM 8.60
CHEMBL254470 IC50 = 3.2 nM 8.49
CHEMBL400467 IC50 = 3.4 nM 8.47
CHEMBL253209 IC50 = 3.7 nM 8.43
CHEMBL252222 IC50 = 5.7 nM 8.24
CHEMBL401002 IC50 = 6.0 nM 8.22
CHEMBL254471 IC50 = 9.0 nM 8.05
CHEMBL253034 IC50 = 19.0 nM 7.72
CHEMBL254055 IC50 = 21.6 nM 7.67
CHEMBL252034 IC50 = 59.0 nM 7.23
CHEMBL253211 IC50 = 60.0 nM 7.22
CHEMBL253666 IC50 = 88.0 nM 7.06
CHEMBL398344 IC50 = 211.0 nM 6.68
CHEMBL252628 IC50 = 238.0 nM 6.62
CHEMBL252610 IC50 = 421.0 nM 6.38
CHEMBL252221 IC50 = 577.0 nM 6.24