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Assay Detail

CHEMBL963306

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

Binding
Binding affinity to CXCR1
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

C-X-C chemokine receptor type 1 (CHEMBL4029)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Fluoroalkyl alpha side chain containing 3,4-diamino-cyclobutenediones as potent and orally bioavailable CXCR2-CXCR1 dual antagonists.
Biju P, Taveras AG, Dwyer MP, Yu Y, Chao J, Hipkin RW, Fan X, Rindgen D, Fine J, Lundell D.
Bioorg Med Chem Lett (2009) 19 : 1431 -1433
PubMed 19196511 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 7.72 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL516184 1 8.30
CHEMBL473959 1 8.22
CHEMBL491330 1 8.22
CHEMBL523984 1 8.22
CHEMBL518857 1 8.10
CHEMBL515262 1 8.05
CHEMBL523645 1 8.00
CHEMBL514001 1 7.80
CHEMBL491135 1 7.70
CHEMBL216981 NAVARIXIN ANHYDROUS 2.0 1 7.70
CHEMBL523437 1 7.66
CHEMBL491487 1 7.62
CHEMBL523769 1 7.60
CHEMBL491506 1 7.52
CHEMBL491134 1 7.47
CHEMBL464301 1 7.40
CHEMBL254370 1 7.40
CHEMBL472749 1 7.37
CHEMBL473145 1 7.00
CHEMBL523807 1 6.99
CHEMBL491312 1 -
CHEMBL473561 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL516184 Ki = 5.0 nM 8.30
CHEMBL473959 Ki = 6.0 nM 8.22
CHEMBL491330 Ki = 6.0 nM 8.22
CHEMBL523984 Ki = 6.0 nM 8.22
CHEMBL518857 Ki = 8.0 nM 8.10
CHEMBL515262 Ki = 9.0 nM 8.05
CHEMBL523645 Ki = 10.0 nM 8.00
CHEMBL514001 Ki = 16.0 nM 7.80
CHEMBL491135 Ki = 20.0 nM 7.70
CHEMBL216981 NAVARIXIN ANHYDROUS Ki = 20.0 nM 7.70
CHEMBL523437 Ki = 22.0 nM 7.66
CHEMBL491487 Ki = 24.0 nM 7.62
CHEMBL523769 Ki = 25.0 nM 7.60
CHEMBL491506 Ki = 30.0 nM 7.52
CHEMBL491134 Ki = 34.0 nM 7.47
CHEMBL464301 Ki = 40.0 nM 7.40
CHEMBL254370 Ki = 40.0 nM 7.40
CHEMBL472749 Ki = 43.0 nM 7.37
CHEMBL473145 Ki = 100.0 nM 7.00
CHEMBL523807 Ki = 103.0 nM 6.99
CHEMBL491312 Ki - -
CHEMBL473561 Ki - -