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Assay Detail

CHEMBL5374239

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

Binding
Inhibition of Cy5-labeled p22phox (149 to 162 residues) probe binding to His-tagged human p47phox (151 to 286 residues) expressed in Escherichia coli BL21 (DE3) pLysS incubated for 10 to 15 mins by fluorescence polarization assay
69
Total Activities
69
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

Neutrophil cytosol factor 1 (CHEMBL1613743)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting NOX2 with Bivalent Small-Molecule p47phox-p22phox Inhibitors.
Zang J, Peters F, Cambet Y, Cifuentes-Pagano E, Hissabu MMS, Dustin CM, Svensson LH, Olesen MM, Poulsen MFL, Jacobsen S, Tuelung PS, Narayanan D, Langkilde AE, Gajhede M, Pagano PJ, Jaquet V, Vilhardt F, Bach A.
J Med Chem (2023) 66 : 14963 -15005
PubMed 37857466 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 69 5.33 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5410142 1 6.62
CHEMBL5427803 1 6.38
CHEMBL5411448 1 6.36
CHEMBL5406295 1 6.33
CHEMBL5412642 1 6.30
CHEMBL5419067 1 6.22
CHEMBL5410678 1 6.19
CHEMBL5413540 1 6.17
CHEMBL5437628 1 6.01
CHEMBL5411421 1 5.91
CHEMBL5398246 1 5.91
CHEMBL5439674 1 5.89
CHEMBL5438922 1 5.88
CHEMBL5439369 1 5.87
CHEMBL5426199 1 5.80
CHEMBL5433544 1 5.79
CHEMBL5429601 1 5.75
CHEMBL5422476 1 5.74
CHEMBL5399098 1 5.73
CHEMBL5406852 1 5.71
CHEMBL5425286 1 5.66
CHEMBL5414953 1 5.59
CHEMBL5437289 1 5.55
CHEMBL5436213 1 5.53
CHEMBL5432879 1 5.50
CHEMBL5421420 1 5.47
CHEMBL5438924 1 5.44
CHEMBL5425482 1 5.44
CHEMBL5404103 1 5.43
CHEMBL5414035 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5410142 Ki = 240.0 nM 6.62
CHEMBL5427803 Ki = 420.0 nM 6.38
CHEMBL5411448 Ki = 440.0 nM 6.36
CHEMBL5406295 Ki = 470.0 nM 6.33
CHEMBL5412642 Ki = 500.0 nM 6.30
CHEMBL5419067 Ki = 600.0 nM 6.22
CHEMBL5410678 Ki = 640.0 nM 6.19
CHEMBL5413540 Ki = 680.0 nM 6.17
CHEMBL5437628 Ki = 980.0 nM 6.01
CHEMBL5411421 Ki = 1230.0 nM 5.91
CHEMBL5398246 Ki = 1220.0 nM 5.91
CHEMBL5439674 Ki = 1290.0 nM 5.89
CHEMBL5438922 Ki = 1320.0 nM 5.88
CHEMBL5439369 Ki = 1360.0 nM 5.87
CHEMBL5426199 Ki = 1580.0 nM 5.80
CHEMBL5433544 Ki = 1640.0 nM 5.79
CHEMBL5429601 Ki = 1770.0 nM 5.75
CHEMBL5422476 Ki = 1820.0 nM 5.74
CHEMBL5399098 Ki = 1880.0 nM 5.73
CHEMBL5406852 Ki = 1930.0 nM 5.71
CHEMBL5425286 Ki = 2170.0 nM 5.66
CHEMBL5414953 Ki = 2580.0 nM 5.59
CHEMBL5437289 Ki = 2840.0 nM 5.55
CHEMBL5436213 Ki = 2940.0 nM 5.53
CHEMBL5432879 Ki = 3180.0 nM 5.50
CHEMBL5421420 Ki = 3370.0 nM 5.47
CHEMBL5425482 Ki = 3630.0 nM 5.44
CHEMBL5438924 Ki = 3620.0 nM 5.44
CHEMBL5404103 Ki = 3740.0 nM 5.43
CHEMBL5414035 Ki = 4250.0 nM 5.37
CHEMBL5437076 Ki = 4900.0 nM 5.31
CHEMBL5421396 Ki = 5500.0 nM 5.26
CHEMBL5416428 Ki = 5720.0 nM 5.24
CHEMBL5412005 Ki = 5920.0 nM 5.23
CHEMBL5427003 Ki = 6310.0 nM 5.20
CHEMBL5440198 Ki = 6340.0 nM 5.20
CHEMBL5422605 Ki = 6390.0 nM 5.19
CHEMBL5437700 Ki = 6780.0 nM 5.17
CHEMBL5399710 Ki = 6850.0 nM 5.16
CHEMBL5422407 Ki = 7580.0 nM 5.12
CHEMBL5429761 Ki = 8400.0 nM 5.08
CHEMBL5418747 Ki = 9440.0 nM 5.03
CHEMBL5400222 Ki = 9530.0 nM 5.02
CHEMBL5399201 Ki = 10100.0 nM 5.00
CHEMBL5415338 Ki = 9900.0 nM 5.00
CHEMBL5422943 Ki = 10100.0 nM 5.00
CHEMBL5407137 Ki = 11100.0 nM 4.96
CHEMBL5437553 Ki = 12300.0 nM 4.91
CHEMBL5415030 Ki = 13000.0 nM 4.89
CHEMBL5412241 Ki = 16800.0 nM 4.78