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Assay Detail

CHEMBL4010335

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

Binding
Inhibition of human DcpS assessed as increase in SMN2 promoter activity
29
Total Activities
29
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

m7GpppX diphosphatase (CHEMBL1949488)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of Potent mRNA Decapping Scavenger Enzyme (DcpS) Inhibitors with Improved Physicochemical Properties To Investigate the Mechanism of Therapeutic Benefit in Spinal Muscular Atrophy (SMA).
Gopalsamy A, Narayanan A, Liu S, Parikh MD, Kyne RE, Fadeyi O, Tones MA, Cherry JJ, Nabhan JF, LaRosa G, Petersen DN, Menard C, Foley TL, Noell S, Ren Y, Loria PM, Maglich-Goodwin J, Rong H, Jones LH.
J Med Chem (2017) 60 : 3094 -3108
PubMed 28257199 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 9.19 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL251906 1 10.70
CHEMBL251428 1 10.70
CHEMBL251429 1 10.52
CHEMBL4080254 1 10.52
CHEMBL4082618 1 10.40
CHEMBL255019 1 10.30
CHEMBL4072132 1 10.16
CHEMBL1232147 1 10.10
CHEMBL4077061 1 9.96
CHEMBL250072 1 9.96
CHEMBL398675 1 9.72
CHEMBL4062544 1 9.60
CHEMBL4061457 1 9.57
CHEMBL399673 1 9.54
CHEMBL4076514 1 9.49
CHEMBL342595 1 9.00
CHEMBL4103454 1 8.86
CHEMBL4068466 1 8.75
CHEMBL4072481 1 8.64
CHEMBL250231 1 8.54
CHEMBL343543 1 8.10
CHEMBL4075292 1 7.98
CHEMBL4100442 1 7.91
CHEMBL4084161 1 7.87
CHEMBL4090641 1 7.79
CHEMBL268354 1 6.85
CHEMBL4093512 1 6.48
CHEMBL4102384 1 -
CHEMBL4075512 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL251906 IC50 = 0.02 nM 10.70
CHEMBL251428 IC50 = 0.02 nM 10.70
CHEMBL251429 IC50 = 0.03 nM 10.52
CHEMBL4080254 IC50 = 0.03 nM 10.52
CHEMBL4082618 IC50 = 0.04 nM 10.40
CHEMBL255019 IC50 = 0.05 nM 10.30
CHEMBL4072132 IC50 = 0.069 nM 10.16
CHEMBL1232147 IC50 = 0.08 nM 10.10
CHEMBL4077061 IC50 = 0.11 nM 9.96
CHEMBL250072 IC50 = 0.11 nM 9.96
CHEMBL398675 IC50 = 0.19 nM 9.72
CHEMBL4062544 IC50 = 0.25 nM 9.60
CHEMBL4061457 IC50 = 0.27 nM 9.57
CHEMBL399673 IC50 = 0.29 nM 9.54
CHEMBL4076514 IC50 = 0.32 nM 9.49
CHEMBL342595 IC50 = 1.01 nM 9.00
CHEMBL4103454 IC50 = 1.39 nM 8.86
CHEMBL4068466 IC50 = 1.77 nM 8.75
CHEMBL4072481 IC50 = 2.3 nM 8.64
CHEMBL250231 IC50 = 2.89 nM 8.54
CHEMBL343543 IC50 = 7.9 nM 8.10
CHEMBL4075292 IC50 = 10.55 nM 7.98
CHEMBL4100442 IC50 = 12.31 nM 7.91
CHEMBL4084161 IC50 = 13.59 nM 7.87
CHEMBL4090641 IC50 = 16.2 nM 7.79
CHEMBL268354 IC50 = 142.58 nM 6.85
CHEMBL4093512 IC50 = 334.3 nM 6.48
CHEMBL4102384 IC50 > 10000.0 nM -
CHEMBL4075512 IC50 > 10000.0 nM -