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Assay Detail

CHEMBL843656

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

Binding
Inhibitory activity against [125I]-MIP-1 alpha binding to human CCR1 receptors.
36
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

C-C chemokine receptor type 1 (CHEMBL2413)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and discovery of a novel CCR1 antagonist.
Naya A, Sagara Y, Ohwaki K, Saeki T, Ichikawa D, Iwasawa Y, Noguchi K, Ohtake N.
J Med Chem (2001) 44 : 1429 -1435
PubMed 11311066 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 7.44 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL277930 4 9.05
CHEMBL289902 1 8.72
CHEMBL34732 1 8.70
CHEMBL32257 1 8.60
CHEMBL33050 1 8.55
CHEMBL418589 1 8.51
CHEMBL33340 1 8.48
CHEMBL33614 1 8.44
CHEMBL33223 1 8.41
CHEMBL32713 1 8.30
CHEMBL280751 1 8.28
CHEMBL33104 1 8.01
CHEMBL34165 1 7.85
CHEMBL33929 1 7.77
CHEMBL34166 BERLEX COMPOUND 1 7.32
CHEMBL33277 1 7.29
CHEMBL33074 1 6.85
CHEMBL33580 1 6.82
CHEMBL34053 1 6.70
CHEMBL33639 1 6.62
CHEMBL33586 1 6.43
CHEMBL34226 1 6.29
CHEMBL33761 1 6.10
CHEMBL285703 1 6.10
CHEMBL286355 1 5.96
CHEMBL33159 1 5.80
CHEMBL289682 1 5.75
CHEMBL433232 1 5.68
CHEMBL32305 1 5.29
CHEMBL286701 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL277930 IC50 = 0.9 nM 9.05
CHEMBL277930 IC50 = 0.9 nM 9.05
CHEMBL277930 IC50 = 1.2 nM 8.92
CHEMBL289902 IC50 = 1.9 nM 8.72
CHEMBL34732 IC50 = 2.0 nM 8.70
CHEMBL32257 IC50 = 2.5 nM 8.60
CHEMBL33050 IC50 = 2.8 nM 8.55
CHEMBL418589 IC50 = 3.1 nM 8.51
CHEMBL33340 IC50 = 3.3 nM 8.48
CHEMBL33614 IC50 = 3.6 nM 8.44
CHEMBL33223 IC50 = 3.9 nM 8.41
CHEMBL32713 IC50 = 5.0 nM 8.30
CHEMBL280751 IC50 = 5.2 nM 8.28
CHEMBL33104 IC50 = 9.7 nM 8.01
CHEMBL34165 IC50 = 14.0 nM 7.85
CHEMBL33929 IC50 = 17.0 nM 7.77
CHEMBL277930 IC50 = 47.0 nM 7.33
CHEMBL34166 BERLEX COMPOUND IC50 = 48.0 nM 7.32
CHEMBL33277 IC50 = 51.0 nM 7.29
CHEMBL33074 IC50 = 140.0 nM 6.85
CHEMBL33580 IC50 = 150.0 nM 6.82
CHEMBL34053 IC50 = 200.0 nM 6.70
CHEMBL33639 IC50 = 240.0 nM 6.62
CHEMBL33586 IC50 = 370.0 nM 6.43
CHEMBL34226 IC50 = 510.0 nM 6.29
CHEMBL33761 IC50 = 800.0 nM 6.10
CHEMBL285703 IC50 = 800.0 nM 6.10
CHEMBL286355 IC50 = 1100.0 nM 5.96
CHEMBL33159 IC50 = 1600.0 nM 5.80
CHEMBL289682 IC50 = 1800.0 nM 5.75
CHEMBL433232 IC50 = 2100.0 nM 5.68
CHEMBL32305 IC50 = 5100.0 nM 5.29
CHEMBL33278 IC50 > 10000.0 nM -
CHEMBL289464 IC50 > 10000.0 nM -
CHEMBL32766 IC50 > 10000.0 nM -
CHEMBL286701 IC50 > 10000.0 nM -