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Assay Detail

CHEMBL2394434

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Binding
Inhibition of KCa2.3 in Sprague-Dawley rat superior cervical ganglion neurons assessed as inhibition of afterhyperpolarization by electrophysiological assay
ChEMBL ↗
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Superior cervical ganglion
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Small conductance calcium-activated potassium channel protein 3 (CHEMBL3780) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Further studies on bis-charged tetraazacyclophanes as potent inhibitors of small conductance Ca(2+)-activated K+ channels.
Yang D, Arifhodzic L, Ganellin CR, Jenkinson DH.
Eur J Med Chem (2013) 63 : 907 -923
PubMed 23685886 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 56 7.82 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2391662 — — 1 8.77
CHEMBL2391665 — — 1 8.64
CHEMBL2391673 — — 1 8.59
CHEMBL185463 — — 1 8.57
CHEMBL2391668 — — 1 8.52
CHEMBL2391675 — — 1 8.52
CHEMBL2391690 — — 1 8.49
CHEMBL2391678 — — 1 8.43
CHEMBL2391826 — — 1 8.42
CHEMBL2391669 — — 1 8.42
CHEMBL2391671 — — 1 8.41
CHEMBL2391666 — — 1 8.40
CHEMBL2391687 — — 1 8.39
CHEMBL2391667 — — 1 8.39
CHEMBL2391664 — — 1 8.39
CHEMBL117908 — — 1 8.39
CHEMBL2391663 — — 1 8.36
CHEMBL2391829 — — 1 8.32
CHEMBL2391677 — — 1 8.29
CHEMBL2391827 — — 1 8.28
CHEMBL2391825 — — 1 8.23
CHEMBL2391670 — — 1 8.17
CHEMBL2391672 — — 1 8.09
CHEMBL3392239 — — 1 8.08
CHEMBL2391660 — — 1 8.01
CHEMBL2391689 — — 1 7.92
CHEMBL2391820 — — 1 7.89
CHEMBL2391817 — — 1 7.85
CHEMBL2391657 — — 1 7.82
CHEMBL2391656 — — 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2391662 — IC50 = 1.7 nM 8.77
CHEMBL2391665 — IC50 = 2.3 nM 8.64
CHEMBL2391673 — IC50 = 2.6 nM 8.59
CHEMBL185463 — IC50 = 2.7 nM 8.57
CHEMBL2391668 — IC50 = 3.0 nM 8.52
CHEMBL2391675 — IC50 = 3.0 nM 8.52
CHEMBL2391690 — IC50 = 3.2 nM 8.49
CHEMBL2391678 — IC50 = 3.7 nM 8.43
CHEMBL2391826 — IC50 = 3.8 nM 8.42
CHEMBL2391669 — IC50 = 3.8 nM 8.42
CHEMBL2391671 — IC50 = 3.9 nM 8.41
CHEMBL2391666 — IC50 = 4.0 nM 8.40
CHEMBL2391667 — IC50 = 4.1 nM 8.39
CHEMBL2391687 — IC50 = 4.1 nM 8.39
CHEMBL2391664 — IC50 = 4.1 nM 8.39
CHEMBL117908 — IC50 = 4.1 nM 8.39
CHEMBL2391663 — IC50 = 4.4 nM 8.36
CHEMBL2391829 — IC50 = 4.8 nM 8.32
CHEMBL2391677 — IC50 = 5.1 nM 8.29
CHEMBL2391827 — IC50 = 5.2 nM 8.28
CHEMBL2391825 — IC50 = 5.9 nM 8.23
CHEMBL2391670 — IC50 = 6.8 nM 8.17
CHEMBL2391672 — IC50 = 8.1 nM 8.09
CHEMBL3392239 — IC50 = 8.3 nM 8.08
CHEMBL2391660 — IC50 = 9.8 nM 8.01
CHEMBL2391689 — IC50 = 12.0 nM 7.92
CHEMBL2391820 — IC50 = 13.0 nM 7.89
CHEMBL2391817 — IC50 = 14.0 nM 7.85
CHEMBL2391657 — IC50 = 15.0 nM 7.82
CHEMBL2391656 — IC50 = 15.0 nM 7.82
CHEMBL2391828 — IC50 = 17.0 nM 7.77
CHEMBL2391683 — IC50 = 17.0 nM 7.77
CHEMBL2391680 — IC50 = 17.0 nM 7.77
CHEMBL2391688 — IC50 = 18.0 nM 7.75
CHEMBL2391659 — IC50 = 19.0 nM 7.72
CHEMBL2391682 — IC50 = 19.0 nM 7.72
CHEMBL2391676 — IC50 = 21.0 nM 7.68
CHEMBL2391681 — IC50 = 21.0 nM 7.68
CHEMBL2391661 — IC50 = 24.0 nM 7.62
CHEMBL2391679 — IC50 = 27.0 nM 7.57
CHEMBL2391818 — IC50 = 33.0 nM 7.48
CHEMBL2391821 — IC50 = 33.0 nM 7.48
CHEMBL2391685 — IC50 = 37.0 nM 7.43
CHEMBL2391686 — IC50 = 42.0 nM 7.38
CHEMBL2391819 — IC50 = 42.0 nM 7.38
CHEMBL2391684 — IC50 = 58.0 nM 7.24
CHEMBL2391658 — IC50 = 76.0 nM 7.12
CHEMBL2391822 — IC50 = 97.0 nM 7.01
CHEMBL2390965 — IC50 = 114.0 nM 6.94
CHEMBL2391814 — IC50 = 124.0 nM 6.91