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

General Information of Drug (ID: DM2T5OV)

• Drug Name: DC-EBIO Drug Info
• Synonyms: dichloro-EBIO

Indication

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

• Cross-matching ID:
  PubChem CID: 656765
  ChEBI ID: CHEBI:34662
  CAS Number: CAS 60563-36-2
  TTD Drug ID: DM2T5OV

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	[7]
UCL1848	DM2CN0A	Discovery agent	N.A.	Investigative	[7]
apamin	DMYNBK5	Discovery agent	N.A.	Investigative	[7]
CyPPA	DM64L9I	Discovery agent	N.A.	Investigative	[8]

Drug(s) Targeting Calcium-activated potassium channel KCa3.1 (KCNN4)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
ICA-17043	DMRFY7I	Alzheimer disease	8A20	Phase 2	[9]
ASP0819	DM6HJ3V	Fibromyalgia	MG30.01	Phase 2	[10]
EBIO	DMPKI0N	Discovery agent	N.A.	Investigative	[6]
1-((2-chlorophenyl)diphenylmethyl)-1H-pyrazole	DMQEJVU	Conjunctival fibrosis	9A61.3	Investigative	[11]
SKA-121	DMBL7YN	Discovery agent	N.A.	Investigative	[12]
PMID15603962Crac-16	DMN5LZQ	Discovery agent	N.A.	Investigative	[13]
SKA-31	DMX34F1	Discovery agent	N.A.	Investigative	[14]

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	[15]
zoxazolamine	DM70TKB	Multiple myeloma	2A83	Terminated	[16]
[14C]TEA	DM6SFYH	Discovery agent	N.A.	Investigative	[6]
EBIO	DMPKI0N	Discovery agent	N.A.	Investigative	[6]
UCL1684	DMZNJFU	Discovery agent	N.A.	Investigative	[17]
UCL1848	DM2CN0A	Discovery agent	N.A.	Investigative	[18]
apamin	DMYNBK5	Discovery agent	N.A.	Investigative	[19]
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 KCa2.2 (KCNN2)	TT2T5M0	KCNN2_HUMAN	Activator	[2]
Calcium-activated potassium channel KCa2.3 (KCNN3)	TT9JH25	KCNN3_HUMAN	Activator	[3]
Calcium-activated potassium channel KCa3.1 (KCNN4)	TT7M9I6	KCNN4_HUMAN	Activator	[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: 2324).
• [2] 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.
• [3] Modulators of small- and intermediate-conductance calcium-activated potassium channels and their therapeutic indications. Curr Med Chem. 2007;14(13):1437-57.
• [4] Benzimidazolone activators of chloride secretion: potential therapeutics for cystic fibrosis and chronic obstructive pulmonary disease. J Pharmacol Exp Ther. 2001 Feb;296(2):600-11.
• [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] 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.
• [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] Senicapoc (ICA-17043): a potential therapy for the prevention and treatment of hemolysis-associated complications in sickle cell anemia.Expert Opin Investig Drugs.2009 Feb;18(2):231-9.
• [10] Efficacy and Safety of ASP0819 in Patients with Fibromyalgia: Results of a Proof-of-Concept, Randomized, Double-Blind, Placebo-Controlled Trial. J Pain Res. 2020 Dec 10;13:3355-3369.
• [11] Blockade of the intermediate-conductance calcium-activated potassium channel as a new therapeutic strategy for restenosis. Circulation. 2003 Sep 2;108(9):1119-25.
• [12] New positive Ca2+-activated K+ channel gating modulators with selectivity for KCa3.1. Mol Pharmacol. 2014 Sep;86(3):342-57.
• [13] IKCa-channel blockers. Part 2: discovery of cyclohexadienes. Bioorg Med Chem Lett. 2005 Jan 17;15(2):401-4.
• [14] Naphtho[1,2-d]thiazol-2-ylamine (SKA-31), a new activator of KCa2 and KCa3.1 potassium channels, potentiates the endothelium-derived hyperpolarizing factor response and lowers blood pressure. Mol Pharmacol. 2009 Feb;75(2):281-95.
• [15] Block of rat brain recombinant SK channels by tricyclic antidepressants and related compounds. Eur J Pharmacol. 2000 Jul 28;401(1):1-7.
• [16] 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.
• [17] 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.
• [18] 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.
• [19] 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.