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Assay Detail

CHEMBL655688

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

Functional
Antagonist activity against C-C chemokine receptor type 2
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

CCR2B receptor antagonists: conversion of a weak HTS hit to a potent lead compound.
Forbes IT, Cooper DG, Dodds EK, Hickey DM, Ife RJ, Meeson M, Stockley M, Berkhout TA, Gohil J, Groot PH, Moores K.
Bioorg Med Chem Lett (2000) 10 : 1803 -1806
PubMed 10969972 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 34 5.96 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL432713 1 7.30
CHEMBL298562 1 7.10
CHEMBL300455 1 6.63
CHEMBL297033 1 6.46
CHEMBL54192 1 6.44
CHEMBL51332 1 6.44
CHEMBL299153 1 6.38
CHEMBL299322 1 6.34
CHEMBL299855 1 6.28
CHEMBL50025 1 6.26
CHEMBL53476 1 6.25
CHEMBL51895 1 6.23
CHEMBL51094 1 6.18
CHEMBL50460 1 6.10
CHEMBL53991 1 6.10
CHEMBL53402 1 6.06
CHEMBL49994 1 5.92
CHEMBL53131 1 5.84
CHEMBL300025 1 5.80
CHEMBL53130 1 5.77
CHEMBL297950 1 5.60
CHEMBL53557 1 5.55
CHEMBL299379 1 5.54
CHEMBL416833 1 5.38
CHEMBL53930 1 5.36
CHEMBL53779 1 5.36
CHEMBL433081 1 5.29
CHEMBL53819 1 5.27
CHEMBL300744 1 5.23
CHEMBL50301 1 5.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL432713 Ki = 50.0 nM 7.30
CHEMBL298562 Ki = 79.0 nM 7.10
CHEMBL300455 Ki = 234.0 nM 6.63
CHEMBL297033 Ki = 350.0 nM 6.46
CHEMBL54192 Ki = 360.0 nM 6.44
CHEMBL51332 Ki = 360.0 nM 6.44
CHEMBL299153 Ki = 420.0 nM 6.38
CHEMBL299322 Ki = 460.0 nM 6.34
CHEMBL299855 Ki = 520.0 nM 6.28
CHEMBL50025 Ki = 550.0 nM 6.26
CHEMBL53476 Ki = 560.0 nM 6.25
CHEMBL51895 Ki = 590.0 nM 6.23
CHEMBL51094 Ki = 660.0 nM 6.18
CHEMBL50460 Ki = 790.0 nM 6.10
CHEMBL53991 Ki = 790.0 nM 6.10
CHEMBL53402 Ki = 870.0 nM 6.06
CHEMBL49994 Ki = 1200.0 nM 5.92
CHEMBL53131 Ki = 1450.0 nM 5.84
CHEMBL300025 Ki = 1600.0 nM 5.80
CHEMBL53130 Ki = 1700.0 nM 5.77
CHEMBL297950 Ki = 2500.0 nM 5.60
CHEMBL53557 Ki = 2800.0 nM 5.55
CHEMBL299379 Ki = 2900.0 nM 5.54
CHEMBL416833 Ki = 4200.0 nM 5.38
CHEMBL53930 Ki = 4400.0 nM 5.36
CHEMBL53779 Ki = 4400.0 nM 5.36
CHEMBL433081 Ki = 5100.0 nM 5.29
CHEMBL53819 Ki = 5400.0 nM 5.27
CHEMBL300744 Ki = 5900.0 nM 5.23
CHEMBL50301 Ki = 6300.0 nM 5.20
CHEMBL52956 Ki = 7100.0 nM 5.15
CHEMBL52435 Ki > 10000.0 nM -
CHEMBL53727 Ki > 10000.0 nM -
CHEMBL300868 Ki > 10000.0 nM -