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Assay Detail

CHEMBL1055928

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

Binding
Displacement of human [125I]IL-8 from human CXCR1
26
Total Activities
26
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-X-C chemokine receptor type 1 (CHEMBL4029)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Diaminocyclobutenediones as potent and orally bioavailable CXCR2 receptor antagonists: SAR in the phenolic amide region.
Aki C, Chao J, Ferreira JA, Dwyer MP, Yu Y, Chao J, Merritt RJ, Lai G, Wu M, Hipkin RW, Fan X, Gonsiorek W, Fosseta J, Rindgen D, Fine J, Lundell D, Taveras AG, Biju P.
Bioorg Med Chem Lett (2009) 19 : 4446 -4449
PubMed 19525110 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 26 6.76 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL556656 1 7.68
CHEMBL556862 1 7.52
CHEMBL254370 1 7.40
CHEMBL562286 1 7.39
CHEMBL563875 1 7.27
CHEMBL561812 1 6.91
CHEMBL385715 1 6.68
CHEMBL562781 1 6.42
CHEMBL550880 1 5.91
CHEMBL562950 1 5.68
CHEMBL550945 1 5.55
CHEMBL563129 1 -
CHEMBL564068 1 -
CHEMBL564029 1 -
CHEMBL563855 1 -
CHEMBL562207 1 -
CHEMBL556861 1 -
CHEMBL562670 1 -
CHEMBL563467 1 -
CHEMBL557466 1 -
CHEMBL563612 1 -
CHEMBL557877 1 -
CHEMBL550130 1 -
CHEMBL560089 1 -
CHEMBL550414 1 -
CHEMBL550006 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL556656 Ki = 21.0 nM 7.68
CHEMBL556862 Ki = 30.0 nM 7.52
CHEMBL254370 Ki = 40.0 nM 7.40
CHEMBL562286 Ki = 41.0 nM 7.39
CHEMBL563875 Ki = 54.0 nM 7.27
CHEMBL561812 Ki = 123.0 nM 6.91
CHEMBL385715 Ki = 210.0 nM 6.68
CHEMBL562781 Ki = 381.0 nM 6.42
CHEMBL550880 Ki = 1221.0 nM 5.91
CHEMBL562950 Ki = 2068.0 nM 5.68
CHEMBL550945 Ki = 2797.0 nM 5.55
CHEMBL563129 Ki - -
CHEMBL564068 Ki - -
CHEMBL564029 Ki - -
CHEMBL563855 Ki - -
CHEMBL562207 Ki - -
CHEMBL556861 Ki - -
CHEMBL562670 Ki - -
CHEMBL563467 Ki - -
CHEMBL557466 Ki - -
CHEMBL563612 Ki - -
CHEMBL557877 Ki - -
CHEMBL550130 Ki > 1000.0 nM -
CHEMBL560089 Ki - -
CHEMBL550414 Ki - -
CHEMBL550006 Ki - -