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Assay Detail

CHEMBL940859

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

Binding
Displacement of [125]MCP1 from CCR2 in human PBMCs
ChEMBL ↗
79
Total Activities
79
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

C-C chemokine receptor type 2 (CHEMBL4015) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Capped diaminopropionamide-glycine dipeptides are inhibitors of CC chemokine receptor 2 (CCR2).
Carter PH, Brown GD, Friedrich SR, Cherney RJ, Tebben AJ, Lo YC, Yang G, Jezak H, Solomon KA, Scherle PA, Decicco CP.
Bioorg Med Chem Lett (2007) 17 : 5455 -5461
PubMed 17720492 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 79 6.65 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL247245 — — 1 7.96
CHEMBL393267 — — 1 7.89
CHEMBL247455 — — 1 7.82
CHEMBL398134 — — 1 7.80
CHEMBL337246 — — 1 7.77
CHEMBL247608 — — 1 7.72
CHEMBL392814 — — 1 7.72
CHEMBL246804 — — 1 7.70
CHEMBL247621 — — 1 7.64
CHEMBL248188 — — 1 7.64
CHEMBL247622 — — 1 7.55
CHEMBL246407 — — 1 7.44
CHEMBL402056 — — 1 7.44
CHEMBL398747 — — 1 7.43
CHEMBL246406 — — 1 7.33
CHEMBL400196 — — 1 7.32
CHEMBL247209 — — 1 7.26
CHEMBL246399 — — 1 7.22
CHEMBL246415 — — 1 7.19
CHEMBL247439 — — 1 7.19
CHEMBL248418 — — 1 7.18
CHEMBL247205 — — 1 7.06
CHEMBL247635 — — 1 7.05
CHEMBL247206 — — 1 7.01
CHEMBL401010 — — 1 7.00
CHEMBL247207 — — 1 7.00
CHEMBL400158 — — 1 6.96
CHEMBL246213 — — 1 6.96
CHEMBL248419 — — 1 6.96
CHEMBL247456 — — 1 6.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL247245 — IC50 = 11.0 nM 7.96
CHEMBL393267 — IC50 = 13.0 nM 7.89
CHEMBL247455 — IC50 = 15.0 nM 7.82
CHEMBL398134 — IC50 = 16.0 nM 7.80
CHEMBL337246 — IC50 = 17.0 nM 7.77
CHEMBL247608 — IC50 = 19.0 nM 7.72
CHEMBL392814 — IC50 = 19.0 nM 7.72
CHEMBL246804 — IC50 = 20.0 nM 7.70
CHEMBL247621 — IC50 = 23.0 nM 7.64
CHEMBL248188 — IC50 = 23.0 nM 7.64
CHEMBL247622 — IC50 = 28.0 nM 7.55
CHEMBL246407 — IC50 = 36.0 nM 7.44
CHEMBL402056 — IC50 = 36.0 nM 7.44
CHEMBL398747 — IC50 = 37.0 nM 7.43
CHEMBL246406 — IC50 = 47.0 nM 7.33
CHEMBL400196 — IC50 = 48.0 nM 7.32
CHEMBL247209 — IC50 = 55.0 nM 7.26
CHEMBL246399 — IC50 = 60.0 nM 7.22
CHEMBL246415 — IC50 = 65.0 nM 7.19
CHEMBL247439 — IC50 = 65.0 nM 7.19
CHEMBL248418 — IC50 = 66.0 nM 7.18
CHEMBL247205 — IC50 = 88.0 nM 7.06
CHEMBL247635 — IC50 = 90.0 nM 7.05
CHEMBL247206 — IC50 = 97.0 nM 7.01
CHEMBL247207 — IC50 = 99.0 nM 7.00
CHEMBL401010 — IC50 = 100.0 nM 7.00
CHEMBL400158 — IC50 = 110.0 nM 6.96
CHEMBL246213 — IC50 = 110.0 nM 6.96
CHEMBL248419 — IC50 = 110.0 nM 6.96
CHEMBL247456 — IC50 = 110.0 nM 6.96
CHEMBL247203 — IC50 = 120.0 nM 6.92
CHEMBL248423 — IC50 = 120.0 nM 6.92
CHEMBL246410 — IC50 = 120.0 nM 6.92
CHEMBL246221 — IC50 = 130.0 nM 6.89
CHEMBL427705 — IC50 = 130.0 nM 6.89
CHEMBL246417 — IC50 = 150.0 nM 6.82
CHEMBL247208 — IC50 = 150.0 nM 6.82
CHEMBL400793 — IC50 = 150.0 nM 6.82
CHEMBL246405 — IC50 = 160.0 nM 6.80
CHEMBL401009 — IC50 = 170.0 nM 6.77
CHEMBL247204 — IC50 = 190.0 nM 6.72
CHEMBL246416 — IC50 = 190.0 nM 6.72
CHEMBL401011 — IC50 = 200.0 nM 6.70
CHEMBL248420 — IC50 = 230.0 nM 6.64
CHEMBL248421 — IC50 = 250.0 nM 6.60
CHEMBL247210 — IC50 = 260.0 nM 6.58
CHEMBL246098 — IC50 = 310.0 nM 6.51
CHEMBL398354 — IC50 = 320.0 nM 6.50
CHEMBL400159 — IC50 = 380.0 nM 6.42
CHEMBL401463 — IC50 = 400.0 nM 6.40