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Assay Detail

CHEMBL3611614

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

Binding
Antagonist activity at human Kv1.1 expressed in HEK293 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 HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Potassium voltage-gated channel subfamily A member 1 (CHEMBL2309) ↗
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 9.96 10.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3609249 — — 1 10.99
CHEMBL3608998 — — 1 10.96
CHEMBL3609244 — — 1 10.96
CHEMBL3609086 — — 1 10.96
CHEMBL3609028 — — 1 10.85
CHEMBL3609089 — — 1 10.82
CHEMBL3609046 — — 1 10.81
CHEMBL3609247 — — 1 10.80
CHEMBL3608317 — — 1 10.76
CHEMBL3609226 — — 1 10.74
CHEMBL3609023 — — 1 10.74
CHEMBL3609044 — — 1 10.71
CHEMBL3609029 — — 1 10.70
CHEMBL3609093 — — 1 10.70
CHEMBL3609268 — — 1 10.59
CHEMBL3609253 — — 1 10.58
CHEMBL3609246 — — 1 10.56
CHEMBL3609242 — — 1 10.55
CHEMBL3609030 — — 1 10.55
CHEMBL3609273 — — 1 10.54
CHEMBL3609269 — — 1 10.49
CHEMBL3609051 — — 1 10.49
CHEMBL3609079 — — 1 10.47
CHEMBL3609264 — — 1 10.40
CHEMBL3609076 — — 1 10.40
CHEMBL3609277 — — 1 10.38
CHEMBL3609040 — — 1 10.34
CHEMBL3609248 — — 1 10.31
CHEMBL3609275 — — 1 10.29
CHEMBL3609072 — — 1 10.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3609249 — IC50 = 0.0102 nM 10.99
CHEMBL3608998 — IC50 = 0.011 nM 10.96
CHEMBL3609244 — IC50 = 0.011 nM 10.96
CHEMBL3609086 — IC50 = 0.011 nM 10.96
CHEMBL3609028 — IC50 = 0.014 nM 10.85
CHEMBL3609089 — IC50 = 0.015 nM 10.82
CHEMBL3609046 — IC50 = 0.0154 nM 10.81
CHEMBL3609247 — IC50 = 0.0157 nM 10.80
CHEMBL3608317 — IC50 = 0.0172 nM 10.76
CHEMBL3609226 — IC50 = 0.0182 nM 10.74
CHEMBL3609023 — IC50 = 0.0181 nM 10.74
CHEMBL3609044 — IC50 = 0.0195 nM 10.71
CHEMBL3609093 — IC50 = 0.02 nM 10.70
CHEMBL3609029 — IC50 = 0.02 nM 10.70
CHEMBL3609268 — IC50 = 0.0256 nM 10.59
CHEMBL3609253 — IC50 = 0.0262 nM 10.58
CHEMBL3609246 — IC50 = 0.0274 nM 10.56
CHEMBL3609030 — IC50 = 0.028 nM 10.55
CHEMBL3609242 — IC50 = 0.028 nM 10.55
CHEMBL3609273 — IC50 = 0.029 nM 10.54
CHEMBL3609051 — IC50 = 0.0324 nM 10.49
CHEMBL3609269 — IC50 = 0.032 nM 10.49
CHEMBL3609079 — IC50 = 0.0335 nM 10.47
CHEMBL3609076 — IC50 = 0.04 nM 10.40
CHEMBL3609264 — IC50 = 0.04 nM 10.40
CHEMBL3609277 — IC50 = 0.042 nM 10.38
CHEMBL3609040 — IC50 = 0.046 nM 10.34
CHEMBL3609248 — IC50 = 0.0489 nM 10.31
CHEMBL3609275 — IC50 = 0.051 nM 10.29
CHEMBL3609072 — IC50 = 0.0527 nM 10.28
CHEMBL3609047 — IC50 = 0.055 nM 10.26
CHEMBL3609056 — IC50 = 0.07 nM 10.15
CHEMBL3609080 — IC50 = 0.075 nM 10.12
CHEMBL3609082 — IC50 = 0.174 nM 9.76
CHEMBL3609081 — IC50 = 0.266 nM 9.57
CHEMBL3609243 — IC50 = 0.305 nM 9.52
CHEMBL3608999 — IC50 = 0.308 nM 9.51
CHEMBL3609234 — IC50 = 0.446 nM 9.35
CHEMBL3609064 — IC50 = 0.458 nM 9.34
CHEMBL3609025 — IC50 = 0.49 nM 9.31
CHEMBL3609059 — IC50 = 0.59 nM 9.23
CHEMBL3609087 — IC50 = 0.6 nM 9.22
CHEMBL3609085 — IC50 = 0.74 nM 9.13
CHEMBL3609228 — IC50 = 0.76 nM 9.12
CHEMBL3609257 — IC50 = 1.018 nM 8.99
CHEMBL3609267 — IC50 = 1.2 nM 8.92
CHEMBL3609031 — IC50 = 1.8 nM 8.74
CHEMBL3609073 — IC50 = 2.342 nM 8.63
CHEMBL3609258 — IC50 = 2.42 nM 8.62
CHEMBL3609039 — IC50 = 3.279 nM 8.48