Target Validation Information
TTD ID	T97947
Target Name	Guanylyl cyclase C (GUCY2C)
Type of Target	Successful
Drug Potency against Target	Linaclotide	Drug Info	EC50 = 400 nM	[1]
Action against Disease Model	Linaclotide	Drug Info	Linaclotide exhibited high affinity and pH-independent binding (K(i): 1.23-1.64 nM) to guanylate cyclase C receptors on h uMan colon carcinoma T84 cells and concomitantly, linaclotide binding resulted in a significant, concentration-dependent acc uMulation of intracellular cyclic guanosine-3', 5'-monophosphate (cGMP) (EC50:99 nM). Linaclotide was stable after 3 h incubation in simulated gastric fluid (pH 1) and similarly, was completely resistant to hydrolysis by pepsin.	[2]
References
REF 1	Positive allosteric modulators of the metabotropic glutamate receptor subtype 2 (mGluR2). Curr Top Med Chem. 2005;5(9):869-84.
REF 2	Linaclotide, through activation of guanylate cyclase C, acts locally in the gastrointestinal tract to elicit enhanced intestinal secretion and transit. Eur J Pharmacol. 2010 Dec 15;649(1-3):328-35.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.