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Assay Detail

CHEMBL1272887

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

Binding
Inhibition of mouse NaV1.8 by electrophysiology
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium channel protein type 10 subunit alpha (CHEMBL5158)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Subtype-selective Na(v)1.8 sodium channel blockers: identification of potent, orally active nicotinamide derivatives.
Kort ME, Atkinson RN, Thomas JB, Drizin I, Johnson MS, Secrest MA, Gregg RJ, Scanio MJ, Shi L, Hakeem AH, Matulenko MA, Chapman ML, Krambis MJ, Liu D, Shieh CC, Zhang X, Simler G, Mikusa JP, Zhong C, Joshi S, Honore P, Roeloffs R, Werness S, Antonio B, Marsh KC, Faltynek CR, Krafte DS, Jarvis MF, Marron BE.
Bioorg Med Chem Lett (2010) 20 : 6812 -6815
PubMed 20855211 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.38 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1270301 1 7.58
CHEMBL1269991 1 7.50
CHEMBL1271106 1 7.24
CHEMBL1269883 1 7.09
CHEMBL1270208 1 7.06
CHEMBL1270207 1 7.06
CHEMBL1271309 1 6.72
CHEMBL1271105 1 6.55
CHEMBL1270797 1 6.54
CHEMBL1270898 1 6.47
CHEMBL1270302 1 6.47
CHEMBL1270999 1 6.40
CHEMBL1271206 1 6.28
CHEMBL1271416 1 6.21
CHEMBL1271417 1 6.21
CHEMBL1270100 1 6.17
CHEMBL1270998 1 6.06
CHEMBL1270899 1 5.85
CHEMBL1271205 1 5.82
CHEMBL1271415 1 5.72
CHEMBL1270099 1 5.58
CHEMBL1270098 1 5.10
CHEMBL1271308 1 4.96
CHEMBL1269882 1 -
CHEMBL1269990 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1270301 IC50 = 26.0 nM 7.58
CHEMBL1269991 IC50 = 32.0 nM 7.50
CHEMBL1271106 IC50 = 57.0 nM 7.24
CHEMBL1269883 IC50 = 81.0 nM 7.09
CHEMBL1270208 IC50 = 87.0 nM 7.06
CHEMBL1270207 IC50 = 88.0 nM 7.06
CHEMBL1271309 IC50 = 190.0 nM 6.72
CHEMBL1271105 IC50 = 280.0 nM 6.55
CHEMBL1270797 IC50 = 290.0 nM 6.54
CHEMBL1270898 IC50 = 340.0 nM 6.47
CHEMBL1270302 IC50 = 340.0 nM 6.47
CHEMBL1270999 IC50 = 400.0 nM 6.40
CHEMBL1271206 IC50 = 530.0 nM 6.28
CHEMBL1271416 IC50 = 610.0 nM 6.21
CHEMBL1271417 IC50 = 620.0 nM 6.21
CHEMBL1270100 IC50 = 680.0 nM 6.17
CHEMBL1270998 IC50 = 870.0 nM 6.06
CHEMBL1270899 IC50 = 1400.0 nM 5.85
CHEMBL1271205 IC50 = 1500.0 nM 5.82
CHEMBL1271415 IC50 = 1900.0 nM 5.72
CHEMBL1270099 IC50 = 2600.0 nM 5.58
CHEMBL1270098 IC50 = 7900.0 nM 5.10
CHEMBL1271308 IC50 = 11000.0 nM 4.96
CHEMBL1269882 IC50 < 30.0 nM -
CHEMBL1269990 IC50 < 30.0 nM -