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Assay Detail

CHEMBL4621458

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Binding
Modulation of human utrophinA expressed in mouse H2K cells assessed as upregulation of utrophin production after 24 hrs by luciferase reporter gene assay
57
Total Activities
55
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

Utrophin (CHEMBL4523230)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-Arylbenzo[<i>d</i>]oxazole Phosphinate Esters as Second-Generation Modulators of Utrophin for the Treatment of Duchenne Muscular Dystrophy.
Babbs A, Berg A, Chatzopoulou M, Davies KE, Davies SG, Edwards B, Elsey DJ, Emer E, Guiraud S, Harriman S, Lecci C, Moir L, Peters D, Robinson N, Rowley JA, Russell AJ, Squire SE, Tinsley JM, Wilson FX, Wynne GM.
J Med Chem (2020) 63 : 7880 -7891
PubMed 32551645 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 57 6.52 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4639067 1 8.40
CHEMBL4639832 1 8.00
CHEMBL4641041 1 7.58
CHEMBL4645628 1 7.47
CHEMBL4637833 1 7.42
CHEMBL4647136 1 7.21
CHEMBL4643175 1 7.15
CHEMBL4638445 1 7.15
CHEMBL4638708 1 7.07
CHEMBL4634557 1 6.97
CHEMBL4636035 1 6.96
CHEMBL4638463 1 6.95
CHEMBL4633264 1 6.93
CHEMBL4638592 3 6.91
CHEMBL4644129 1 6.84
CHEMBL4637813 1 6.83
CHEMBL4644346 1 6.80
CHEMBL4633235 1 6.79
CHEMBL4635899 1 6.79
CHEMBL4638950 1 6.78
CHEMBL1773683 EZUTROMID 2.0 1 6.73
CHEMBL4646007 1 6.70
CHEMBL4636283 1 6.63
CHEMBL4645547 1 6.61
CHEMBL4647847 1 6.52
CHEMBL4646025 1 6.48
CHEMBL4640211 1 6.26
CHEMBL4648719 1 6.12
CHEMBL4633558 1 6.11
CHEMBL4646039 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4639067 EC50 = 4.0 nM 8.40
CHEMBL4639832 EC50 = 10.0 nM 8.00
CHEMBL4641041 EC50 = 26.0 nM 7.58
CHEMBL4645628 EC50 = 34.0 nM 7.47
CHEMBL4637833 EC50 = 38.0 nM 7.42
CHEMBL4647136 EC50 = 62.0 nM 7.21
CHEMBL4638445 EC50 = 71.0 nM 7.15
CHEMBL4643175 EC50 = 71.0 nM 7.15
CHEMBL4638708 EC50 = 85.0 nM 7.07
CHEMBL4634557 EC50 = 108.0 nM 6.97
CHEMBL4636035 EC50 = 110.0 nM 6.96
CHEMBL4638463 EC50 = 112.0 nM 6.95
CHEMBL4633264 EC50 = 118.0 nM 6.93
CHEMBL4638592 EC50 = 124.0 nM 6.91
CHEMBL4644129 EC50 = 146.0 nM 6.84
CHEMBL4637813 EC50 = 148.0 nM 6.83
CHEMBL4644346 EC50 = 157.0 nM 6.80
CHEMBL4635899 EC50 = 164.0 nM 6.79
CHEMBL4633235 EC50 = 163.0 nM 6.79
CHEMBL4638950 EC50 = 168.0 nM 6.78
CHEMBL1773683 EZUTROMID EC50 = 187.0 nM 6.73
CHEMBL4646007 EC50 = 198.0 nM 6.70
CHEMBL4636283 EC50 = 234.0 nM 6.63
CHEMBL4638592 EC50 = 244.0 nM 6.61
CHEMBL4645547 EC50 = 244.0 nM 6.61
CHEMBL4647847 EC50 = 303.0 nM 6.52
CHEMBL4646025 EC50 = 332.0 nM 6.48
CHEMBL4640211 EC50 = 548.0 nM 6.26
CHEMBL4638592 EC50 = 711.0 nM 6.15
CHEMBL4648719 EC50 = 766.0 nM 6.12
CHEMBL4633558 EC50 = 777.0 nM 6.11
CHEMBL4633134 EC50 = 826.0 nM 6.08
CHEMBL4646039 EC50 = 823.0 nM 6.08
CHEMBL4642259 EC50 = 861.0 nM 6.07
CHEMBL4638605 EC50 = 928.0 nM 6.03
CHEMBL4634003 EC50 = 1140.0 nM 5.94
CHEMBL4641107 EC50 = 1140.0 nM 5.94
CHEMBL4634760 EC50 = 1190.0 nM 5.92
CHEMBL4644181 EC50 = 1230.0 nM 5.91
CHEMBL4640452 EC50 = 1250.0 nM 5.90
CHEMBL4634268 EC50 = 1280.0 nM 5.89
CHEMBL4635233 EC50 = 1510.0 nM 5.82
CHEMBL4637613 EC50 = 1510.0 nM 5.82
CHEMBL4638190 EC50 = 1770.0 nM 5.75
CHEMBL4648266 EC50 = 1760.0 nM 5.75
CHEMBL4636645 EC50 = 1770.0 nM 5.75
CHEMBL4646254 EC50 = 1760.0 nM 5.75
CHEMBL4635679 EC50 = 1950.0 nM 5.71
CHEMBL4637665 EC50 = 2250.0 nM 5.65
CHEMBL4641851 EC50 - -