Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMYNBK5)

• Drug Name: apamin Drug Info
• Synonyms: 08APA001_SMARTOX; GTPL2311; 08APA001; Apamin, synthetic, > Apamin, from bee venom, &gt

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 16218850
  TTD Drug ID: DMYNBK5
  VARIDT Drug ID: DR00806

Molecule-Related Drug Atlas

Drug(s) Targeting Calcium-activated potassium channel KCa2.3 (KCNN3)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
dequalinium	DMXM19W	Myelopathy	8B42	Clinical trial	[5]
[14C]TEA	DM6SFYH	Discovery agent	N.A.	Investigative	[6]
EBIO	DMPKI0N	Discovery agent	N.A.	Investigative	[6]
UCL1684	DMZNJFU	Discovery agent	N.A.	Investigative	[4]
DC-EBIO	DM2T5OV	Discovery agent	N.A.	Investigative	[7]
UCL1848	DM2CN0A	Discovery agent	N.A.	Investigative	[4]
CyPPA	DM64L9I	Discovery agent	N.A.	Investigative	[8]

Drug(s) Targeting Calcium-activated potassium channel KCa2.1 (KCNN1)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
dequalinium	DMXM19W	Myelopathy	8B42	Clinical trial	[2]
[14C]TEA	DM6SFYH	Discovery agent	N.A.	Investigative	[6]
EBIO	DMPKI0N	Discovery agent	N.A.	Investigative	[6]
UCL1684	DMZNJFU	Discovery agent	N.A.	Investigative	[6]
UCL1848	DM2CN0A	Discovery agent	N.A.	Investigative	[9]

Drug(s) Targeting Calcium-activated potassium channel KCa2.2 (KCNN2)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
dequalinium	DMXM19W	Myelopathy	8B42	Clinical trial	[10]
zoxazolamine	DM70TKB	Multiple myeloma	2A83	Terminated	[11]
[14C]TEA	DM6SFYH	Discovery agent	N.A.	Investigative	[6]
EBIO	DMPKI0N	Discovery agent	N.A.	Investigative	[6]
UCL1684	DMZNJFU	Discovery agent	N.A.	Investigative	[2]
DC-EBIO	DM2T5OV	Discovery agent	N.A.	Investigative	[12]
UCL1848	DM2CN0A	Discovery agent	N.A.	Investigative	[13]
CyPPA	DM64L9I	Discovery agent	N.A.	Investigative	[8]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Calcium-activated potassium channel KCa2.1 (KCNN1)	TT9R6BE	KCNN1_HUMAN	Blocker (channel blocker)	[2]
Calcium-activated potassium channel KCa2.2 (KCNN2)	TT2T5M0	KCNN2_HUMAN	Blocker (channel blocker)	[3]
Calcium-activated potassium channel KCa2.3 (KCNN3)	TT9JH25	KCNN3_HUMAN	Blocker (channel blocker)	[4]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2311).
• [2] Pharmacological characterization of small-conductance Ca(2+)-activated K(+) channels stably expressed in HEK 293 cells. Br J Pharmacol. 2000 Mar;129(5):991-9.
• [3] SK2 encodes the apamin-sensitive Ca(2+)-activated K(+) channels in the human leukemic T cell line, Jurkat. FEBS Lett. 2000 Mar 10;469(2-3):196-202.
• [4] SK3 is an important component of K(+) channels mediating the afterhyperpolarization in cultured rat SCG neurones. J Physiol. 2001 Sep 1;535(Pt 2):323-34.
• [5] Pharmacological characterisation of the human small conductance calcium-activated potassium channel hSK3 reveals sensitivity to tricyclic antidepressants and antipsychotic phenothiazines. Neuropharmacology. 2001 May;40(6):772-83.
• [6] Small conductance calcium-activated potassium channels: from structure to function. Prog Neurobiol. 2010 Jul;91(3):242-55.
• [7] Modulators of small- and intermediate-conductance calcium-activated potassium channels and their therapeutic indications. Curr Med Chem. 2007;14(13):1437-57.
• [8] Selective positive modulation of the SK3 and SK2 subtypes of small conductance Ca2+-activated K+ channels. Br J Pharmacol. 2007 Jul;151(5):655-65.
• [9] The pharmacology of hSK1 Ca2+-activated K+ channels expressed in mammalian cell lines. Br J Pharmacol. 2000 Feb;129(4):627-30.
• [10] Block of rat brain recombinant SK channels by tricyclic antidepressants and related compounds. Eur J Pharmacol. 2000 Jul 28;401(1):1-7.
• [11] Modulation of recombinant small-conductance Ca(2+)-activated K(+) channels by the muscle relaxant chlorzoxazone and structurally related compounds. J Pharmacol Exp Ther. 2001 Mar;296(3):683-9.
• [12] Specific enhancement of SK channel activity selectively potentiates the afterhyperpolarizing current I(AHP) and modulates the firing properties of ... J Biol Chem. 2005 Dec 16;280(50):41404-11.
• [13] Calcium-activated potassium channels sustain calcium signaling in T lymphocytes. Selective blockers and manipulated channel expression levels. J Biol Chem. 2001 Apr 13;276(15):12249-56.