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Assay Detail

CHEMBL3611613

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

Binding
Antagonist activity at human Kv1.3 expressed in CHOK1 cells assessed as inhibition of potassium currents after 10 mins by IonWorks Quattro patch clamp electrophysiology assay
ChEMBL ↗
141
Total Activities
141
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Potassium voltage-gated channel subfamily A member 3 (CHEMBL4633) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pharmaceutical Optimization of Peptide Toxins for Ion Channel Targets: Potent, Selective, and Long-Lived Antagonists of Kv1.3.
Murray JK, Qian YX, Liu B, Elliott R, Aral J, Park C, Zhang X, Stenkilsson M, Salyers K, Rose M, Li H, Yu S, Andrews KL, Colombero A, Werner J, Gaida K, Sickmier EA, Miu P, Itano A, McGivern J, Gegg CV, Sullivan JK, Miranda LP.
J Med Chem (2015) 58 : 6784 -6802
PubMed 26288216 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 141 9.77 10.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3609058 — — 1 10.42
CHEMBL3609248 — — 1 10.41
CHEMBL3609236 — — 1 10.41
CHEMBL3609089 — — 1 10.40
CHEMBL3609035 — — 1 10.22
CHEMBL3609088 — — 1 10.22
CHEMBL3609230 — — 1 10.21
CHEMBL3609036 — — 1 10.17
CHEMBL3609077 — — 1 10.17
CHEMBL3609234 — — 1 10.15
CHEMBL3609092 — — 1 10.15
CHEMBL3609071 — — 1 10.14
CHEMBL3609043 — — 1 10.14
CHEMBL3609249 — — 1 10.14
CHEMBL3609037 — — 1 10.13
CHEMBL3609266 — — 1 10.12
CHEMBL3609237 — — 1 10.12
CHEMBL3609263 — — 1 10.11
CHEMBL3609045 — — 1 10.10
CHEMBL3608997 — — 1 10.10
CHEMBL3609086 — — 1 10.09
CHEMBL3609067 — — 1 10.08
CHEMBL3609222 — — 1 10.07
CHEMBL3609046 — — 1 10.06
CHEMBL3609049 — — 1 10.02
CHEMBL3609042 — — 1 10.02
CHEMBL3609265 — — 1 10.02
CHEMBL3609270 — — 1 10.01
CHEMBL3609078 — — 1 10.00
CHEMBL3609256 — — 1 9.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3609058 — IC50 = 0.038 nM 10.42
CHEMBL3609236 — IC50 = 0.039 nM 10.41
CHEMBL3609248 — IC50 = 0.039 nM 10.41
CHEMBL3609089 — IC50 = 0.04 nM 10.40
CHEMBL3609088 — IC50 = 0.06 nM 10.22
CHEMBL3609035 — IC50 = 0.06 nM 10.22
CHEMBL3609230 — IC50 = 0.062 nM 10.21
CHEMBL3609077 — IC50 = 0.067 nM 10.17
CHEMBL3609036 — IC50 = 0.067 nM 10.17
CHEMBL3609092 — IC50 = 0.071 nM 10.15
CHEMBL3609234 — IC50 = 0.07 nM 10.15
CHEMBL3609071 — IC50 = 0.073 nM 10.14
CHEMBL3609249 — IC50 = 0.073 nM 10.14
CHEMBL3609043 — IC50 = 0.073 nM 10.14
CHEMBL3609037 — IC50 = 0.074 nM 10.13
CHEMBL3609237 — IC50 = 0.075 nM 10.12
CHEMBL3609266 — IC50 = 0.075 nM 10.12
CHEMBL3609263 — IC50 = 0.077 nM 10.11
CHEMBL3608997 — IC50 = 0.079 nM 10.10
CHEMBL3609045 — IC50 = 0.079 nM 10.10
CHEMBL3609086 — IC50 = 0.082 nM 10.09
CHEMBL3609067 — IC50 = 0.083 nM 10.08
CHEMBL3609222 — IC50 = 0.085 nM 10.07
CHEMBL3609046 — IC50 = 0.088 nM 10.06
CHEMBL3609265 — IC50 = 0.095 nM 10.02
CHEMBL3609042 — IC50 = 0.096 nM 10.02
CHEMBL3609049 — IC50 = 0.095 nM 10.02
CHEMBL3609270 — IC50 = 0.097 nM 10.01
CHEMBL3609078 — IC50 = 0.1 nM 10.00
CHEMBL3609256 — IC50 = 0.103 nM 9.99
CHEMBL3609048 — IC50 = 0.104 nM 9.98
CHEMBL3609055 — IC50 = 0.107 nM 9.97
CHEMBL3609038 — IC50 = 0.11 nM 9.96
CHEMBL3609022 — IC50 = 0.11 nM 9.96
CHEMBL3609231 — IC50 = 0.115 nM 9.94
CHEMBL3608998 — IC50 = 0.119 nM 9.92
CHEMBL3609276 — IC50 = 0.12 nM 9.92
CHEMBL3609079 — IC50 = 0.122 nM 9.91
CHEMBL3609083 — IC50 = 0.122 nM 9.91
CHEMBL3609261 — IC50 = 0.126 nM 9.90
CHEMBL3609090 — IC50 = 0.13 nM 9.89
CHEMBL3609065 — IC50 = 0.129 nM 9.89
CHEMBL3609093 — IC50 = 0.132 nM 9.88
CHEMBL3609238 — IC50 = 0.133 nM 9.88
CHEMBL3609272 — IC50 = 0.133 nM 9.88
CHEMBL3609069 — IC50 = 0.133 nM 9.88
CHEMBL3609232 — IC50 = 0.135 nM 9.87
CHEMBL3609032 — IC50 = 0.143 nM 9.85
CHEMBL3609085 — IC50 = 0.14 nM 9.85
CHEMBL3609054 — IC50 = 0.146 nM 9.84