Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4037524

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

Binding
Antagonist activity at TEV protease cleavage site linked GAL4-VP16-fused recombinant human CXCR2 expressed in cells assessed as inhibition of TEV protease tagged human CXCL1-stimulated beta-arrestin recruitment by CCF4-AM-fluorescence based FRET assay
ChEMBL ↗
68
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

C-X-C chemokine receptor type 2 (CHEMBL2434) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Novel 1-Cyclopentenyl-3-phenylureas as Selective, Brain Penetrant, and Orally Bioavailable CXCR2 Antagonists.
Lu H, Yang T, Xu Z, Lin X, Ding Q, Zhang Y, Cai X, Dong K, Gong S, Zhang W, Patel M, Copley RCB, Xiang J, Guan X, Wren P, Ren F.
J Med Chem (2018) 61 : 2518 -2532
PubMed 29406702 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 68 8.26 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4066904 — — 1 9.80
CHEMBL4098864 — — 1 9.70
CHEMBL4082136 — — 1 9.70
CHEMBL4062361 — — 1 9.60
CHEMBL4072270 — — 1 9.60
CHEMBL4060139 — — 1 9.60
CHEMBL4077201 — — 1 9.50
CHEMBL3817901 — — 1 9.40
CHEMBL4070506 — — 1 9.40
CHEMBL4086957 — — 1 9.40
CHEMBL4066818 — — 1 9.40
CHEMBL4103349 — — 1 9.30
CHEMBL4082031 — — 1 9.30
CHEMBL4066510 — — 1 9.30
CHEMBL4088551 — — 1 9.30
CHEMBL4098979 — — 1 9.20
CHEMBL4079102 — — 1 9.20
CHEMBL4089421 — — 1 9.10
CHEMBL4067429 — — 2 9.00
CHEMBL4095602 — — 1 9.00
CHEMBL4076053 — — 1 9.00
CHEMBL4076428 — — 1 9.00
CHEMBL4097602 — — 1 9.00
CHEMBL4094324 — — 1 9.00
CHEMBL4100674 — — 1 9.00
CHEMBL4076478 — — 1 8.90
CHEMBL4062546 — — 1 8.90
CHEMBL4079718 — — 1 8.90
CHEMBL4084077 — — 1 8.90
CHEMBL4081963 — — 1 8.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4066904 — IC50 = 0.1585 nM 9.80
CHEMBL4082136 — IC50 = 0.1995 nM 9.70
CHEMBL4098864 — IC50 = 0.1995 nM 9.70
CHEMBL4072270 — IC50 = 0.2512 nM 9.60
CHEMBL4062361 — IC50 = 0.2512 nM 9.60
CHEMBL4060139 — IC50 = 0.2512 nM 9.60
CHEMBL4077201 — IC50 = 0.3162 nM 9.50
CHEMBL3817901 — IC50 = 0.3981 nM 9.40
CHEMBL4070506 — IC50 = 0.3981 nM 9.40
CHEMBL4086957 — IC50 = 0.3981 nM 9.40
CHEMBL4066818 — IC50 = 0.3981 nM 9.40
CHEMBL4066510 — IC50 = 0.5012 nM 9.30
CHEMBL4088551 — IC50 = 0.5012 nM 9.30
CHEMBL4082031 — IC50 = 0.5012 nM 9.30
CHEMBL4103349 — IC50 = 0.5012 nM 9.30
CHEMBL4098979 — IC50 = 0.631 nM 9.20
CHEMBL4079102 — IC50 = 0.631 nM 9.20
CHEMBL4089421 — IC50 = 0.7943 nM 9.10
CHEMBL4094324 — IC50 = 1.0 nM 9.00
CHEMBL4097602 — IC50 = 1.0 nM 9.00
CHEMBL4076428 — IC50 = 1.0 nM 9.00
CHEMBL4095602 — IC50 = 1.0 nM 9.00
CHEMBL4100674 — IC50 = 1.0 nM 9.00
CHEMBL4067429 — IC50 = 1.0 nM 9.00
CHEMBL4076053 — IC50 = 1.0 nM 9.00
CHEMBL4062546 — IC50 = 1.259 nM 8.90
CHEMBL4076478 — IC50 = 1.259 nM 8.90
CHEMBL4079718 — IC50 = 1.259 nM 8.90
CHEMBL4084077 — IC50 = 1.259 nM 8.90
CHEMBL4081963 — IC50 = 1.585 nM 8.80
CHEMBL4098536 — IC50 = 1.585 nM 8.80
CHEMBL4084135 — IC50 = 1.585 nM 8.80
CHEMBL4072010 — IC50 = 1.995 nM 8.70
CHEMBL4060060 — IC50 = 1.995 nM 8.70
CHEMBL4076676 — IC50 = 2.512 nM 8.60
CHEMBL4071499 — IC50 = 3.162 nM 8.50
CHEMBL4092148 — IC50 = 3.981 nM 8.40
CHEMBL4089896 — IC50 = 3.981 nM 8.40
CHEMBL4067429 — IC50 = 5.2 nM 8.28
CHEMBL4084412 — IC50 = 6.31 nM 8.20
CHEMBL4093313 — IC50 = 10.0 nM 8.00
CHEMBL4071768 — IC50 = 10.0 nM 8.00
CHEMBL4068799 — IC50 = 10.0 nM 8.00
CHEMBL4090813 — IC50 = 10.0 nM 8.00
CHEMBL4064349 — IC50 = 10.0 nM 8.00
CHEMBL4062881 — IC50 = 12.59 nM 7.90
CHEMBL4064083 — IC50 = 25.12 nM 7.60
CHEMBL4091344 — IC50 = 25.12 nM 7.60
CHEMBL4070629 — IC50 = 31.62 nM 7.50
CHEMBL4085657 — IC50 = 39.81 nM 7.40