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Assay Detail

CHEMBL3419344

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

Binding
Inhibition of human NaV1.4 at -140 mV holding potential by whole-cell patch clamp assay
ChEMBL ↗
70
Total Activities
70
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

Sodium channel protein type 4 subunit alpha (CHEMBL2072) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Engineering potent and selective analogues of GpTx-1, a tarantula venom peptide antagonist of the Na(V)1.7 sodium channel.
Murray JK, Ligutti J, Liu D, Zou A, Poppe L, Li H, Andrews KL, Moyer BD, McDonough SI, Favreau P, Stöcklin R, Miranda LP.
J Med Chem (2015) 58 : 2299 -2314
PubMed 25658507 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 70 5.88 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4524078 — — 1 7.70
CHEMBL3318132 — — 1 7.52
CHEMBL3416931 — — 1 7.16
CHEMBL3416933 — — 1 7.05
CHEMBL3416926 — — 1 7.00
CHEMBL3416930 — — 1 7.00
CHEMBL3416944 — — 1 6.96
CHEMBL3416937 — — 1 6.96
CHEMBL3416934 — — 1 6.85
CHEMBL3416886 — — 1 6.70
CHEMBL3416936 — — 1 6.62
CHEMBL3416946 — — 1 6.62
CHEMBL3416932 — — 1 6.39
CHEMBL3416942 — — 1 6.30
CHEMBL3416943 — — 1 6.28
CHEMBL3416940 — — 1 6.13
CHEMBL3417035 — — 1 6.10
CHEMBL3416921 — — 1 6.05
CHEMBL3416923 — — 1 6.05
CHEMBL3416898 — — 1 6.05
CHEMBL3416929 — — 1 5.96
CHEMBL3417038 — — 1 5.92
CHEMBL3416928 — — 1 5.82
CHEMBL3416902 — — 1 5.82
CHEMBL3416927 — — 1 5.77
CHEMBL3416890 — — 1 5.75
CHEMBL3417041 — — 1 5.72
CHEMBL3416906 — — 1 5.72
CHEMBL3416922 — — 1 5.70
CHEMBL3416938 — — 1 5.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4524078 — IC50 = 20.0 nM 7.70
CHEMBL3318132 — IC50 = 30.0 nM 7.52
CHEMBL3416931 — IC50 = 70.0 nM 7.16
CHEMBL3416933 — IC50 = 90.0 nM 7.05
CHEMBL3416926 — IC50 = 100.0 nM 7.00
CHEMBL3416930 — IC50 = 100.0 nM 7.00
CHEMBL3416944 — IC50 = 110.0 nM 6.96
CHEMBL3416937 — IC50 = 110.0 nM 6.96
CHEMBL3416934 — IC50 = 140.0 nM 6.85
CHEMBL3416886 — IC50 = 200.0 nM 6.70
CHEMBL3416936 — IC50 = 240.0 nM 6.62
CHEMBL3416946 — IC50 = 240.0 nM 6.62
CHEMBL3416932 — IC50 = 410.0 nM 6.39
CHEMBL3416942 — IC50 = 500.0 nM 6.30
CHEMBL3416943 — IC50 = 530.0 nM 6.28
CHEMBL3416940 — IC50 = 740.0 nM 6.13
CHEMBL3417035 — IC50 = 800.0 nM 6.10
CHEMBL3416921 — IC50 = 900.0 nM 6.05
CHEMBL3416923 — IC50 = 900.0 nM 6.05
CHEMBL3416898 — IC50 = 900.0 nM 6.05
CHEMBL3416929 — IC50 = 1100.0 nM 5.96
CHEMBL3417038 — IC50 = 1200.0 nM 5.92
CHEMBL3416928 — IC50 = 1500.0 nM 5.82
CHEMBL3416902 — IC50 = 1500.0 nM 5.82
CHEMBL3416927 — IC50 = 1700.0 nM 5.77
CHEMBL3416890 — IC50 = 1800.0 nM 5.75
CHEMBL3416906 — IC50 = 1900.0 nM 5.72
CHEMBL3417041 — IC50 = 1900.0 nM 5.72
CHEMBL3416922 — IC50 = 2000.0 nM 5.70
CHEMBL3416938 — IC50 = 2600.0 nM 5.58
CHEMBL3416899 — IC50 = 2700.0 nM 5.57
CHEMBL3416896 — IC50 = 3000.0 nM 5.52
CHEMBL3416897 — IC50 = 3000.0 nM 5.52
CHEMBL3416901 — IC50 = 3000.0 nM 5.52
CHEMBL3416904 — IC50 = 3000.0 nM 5.52
CHEMBL3416892 — IC50 = 3200.0 nM 5.50
CHEMBL3416908 — IC50 = 3200.0 nM 5.50
CHEMBL3417039 — IC50 = 3300.0 nM 5.48
CHEMBL3416935 — IC50 = 3400.0 nM 5.47
CHEMBL3416905 — IC50 = 3700.0 nM 5.43
CHEMBL3416894 — IC50 = 3800.0 nM 5.42
CHEMBL4524054 — IC50 = 3900.0 nM 5.41
CHEMBL3416920 — IC50 = 4100.0 nM 5.39
CHEMBL3416909 — IC50 = 4100.0 nM 5.39
CHEMBL3416914 — IC50 = 4500.0 nM 5.35
CHEMBL3416919 — IC50 = 4600.0 nM 5.34
CHEMBL3416925 — IC50 = 4700.0 nM 5.33
CHEMBL3416900 — IC50 = 4700.0 nM 5.33
CHEMBL3416945 — IC50 = 4900.0 nM 5.31
CHEMBL3416941 — IC50 = 6100.0 nM 5.21