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Assay Detail

CHEMBL3611617

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

Binding
Antagonist activity at Kv1.3 in human whole blood assessed as inhibition of thapsigargin-induced IFN-gamma secretion incubated for 30 prior to thapsigargin induction measured after 48 hrs by electrochemilluminescent immunoassay
ChEMBL ↗
143
Total Activities
143
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Blood
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 143 9.30 10.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3609265 — — 1 10.41
CHEMBL3609033 — — 1 10.37
CHEMBL3608994 — — 1 10.34
CHEMBL3609095 — — 1 10.34
CHEMBL3609224 — — 1 10.32
CHEMBL3609093 — — 1 10.32
CHEMBL3609266 — — 1 10.30
CHEMBL3609063 — — 1 10.27
CHEMBL3609272 — — 1 10.26
CHEMBL3609271 — — 1 10.25
CHEMBL3609048 — — 1 10.25
CHEMBL3609058 — — 1 10.24
CHEMBL3609263 — — 1 10.20
CHEMBL3608997 — — 1 10.18
CHEMBL3609081 — — 1 10.15
CHEMBL3608995 — — 1 10.15
CHEMBL3609062 — — 1 10.14
CHEMBL3608993 — — 1 10.09
CHEMBL3608998 — — 1 10.09
CHEMBL3609068 — — 1 10.09
CHEMBL3609238 — — 1 10.08
CHEMBL3609256 — — 1 10.08
CHEMBL3609276 — — 1 10.08
CHEMBL3609042 — — 1 10.08
CHEMBL3609223 — — 1 10.05
CHEMBL3609074 — — 1 10.05
CHEMBL3609054 — — 1 10.03
CHEMBL3609077 — — 1 9.97
CHEMBL3608992 — — 1 9.96
CHEMBL3609248 — — 1 9.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3609265 — IC50 = 0.039 nM 10.41
CHEMBL3609033 — IC50 = 0.043 nM 10.37
CHEMBL3608994 — IC50 = 0.046 nM 10.34
CHEMBL3609095 — IC50 = 0.046 nM 10.34
CHEMBL3609093 — IC50 = 0.048 nM 10.32
CHEMBL3609224 — IC50 = 0.048 nM 10.32
CHEMBL3609266 — IC50 = 0.05 nM 10.30
CHEMBL3609063 — IC50 = 0.054 nM 10.27
CHEMBL3609272 — IC50 = 0.055 nM 10.26
CHEMBL3609048 — IC50 = 0.056 nM 10.25
CHEMBL3609271 — IC50 = 0.056 nM 10.25
CHEMBL3609058 — IC50 = 0.058 nM 10.24
CHEMBL3609263 — IC50 = 0.063 nM 10.20
CHEMBL3608997 — IC50 = 0.066 nM 10.18
CHEMBL3608995 — IC50 = 0.07 nM 10.15
CHEMBL3609081 — IC50 = 0.071 nM 10.15
CHEMBL3609062 — IC50 = 0.073 nM 10.14
CHEMBL3608993 — IC50 = 0.081 nM 10.09
CHEMBL3609068 — IC50 = 0.082 nM 10.09
CHEMBL3608998 — IC50 = 0.081 nM 10.09
CHEMBL3609238 — IC50 = 0.083 nM 10.08
CHEMBL3609042 — IC50 = 0.083 nM 10.08
CHEMBL3609276 — IC50 = 0.083 nM 10.08
CHEMBL3609256 — IC50 = 0.084 nM 10.08
CHEMBL3609223 — IC50 = 0.09 nM 10.05
CHEMBL3609074 — IC50 = 0.089 nM 10.05
CHEMBL3609054 — IC50 = 0.094 nM 10.03
CHEMBL3609077 — IC50 = 0.108 nM 9.97
CHEMBL3608992 — IC50 = 0.111 nM 9.96
CHEMBL3609268 — IC50 = 0.109 nM 9.96
CHEMBL3609248 — IC50 = 0.11 nM 9.96
CHEMBL3609037 — IC50 = 0.116 nM 9.94
CHEMBL3609232 — IC50 = 0.12 nM 9.92
CHEMBL3609038 — IC50 = 0.123 nM 9.91
CHEMBL3609036 — IC50 = 0.124 nM 9.91
CHEMBL3609237 — IC50 = 0.122 nM 9.91
CHEMBL3609261 — IC50 = 0.129 nM 9.89
CHEMBL3609043 — IC50 = 0.129 nM 9.89
CHEMBL3609022 — IC50 = 0.132 nM 9.88
CHEMBL3609084 — IC50 = 0.136 nM 9.87
CHEMBL3609260 — IC50 = 0.148 nM 9.83
CHEMBL3609073 — IC50 = 0.151 nM 9.82
CHEMBL3609085 — IC50 = 0.16 nM 9.80
CHEMBL3609222 — IC50 = 0.158 nM 9.80
CHEMBL3609035 — IC50 = 0.176 nM 9.75
CHEMBL3609046 — IC50 = 0.183 nM 9.74
CHEMBL3609230 — IC50 = 0.186 nM 9.73
CHEMBL3609075 — IC50 = 0.193 nM 9.71
CHEMBL3609055 — IC50 = 0.194 nM 9.71
CHEMBL3609071 — IC50 = 0.201 nM 9.70