Patent ID: 7901893

Claim:
A method for identifying a ligand of NPC1L1 comprising: (a) contacting human NPC1L1 with a candidate compound and a detectably labeled substituted 2-azetidinone glucuronide compound selected from the group consisting of compound 1, compound 8 and a compound of Formula II a wherein, R 9 is selected from the group consisting of —C≡C—CH 2 —NR 10 R 11 wherein R 11 is selected from the group consisting of —H, —C 1-3 alkyl, —C(O)—C 1-3 alkyl, —C(O)—NR 10 R 10 , —SO 2 —C 1-3 alkyl and —SO 2 -phenyl; —C≡C(O)NR 10 —SO 2 —C 1-3 alkyl; —C≡C—C(O)NR 10 —SO 2 —phenyl; —(CH 2 ) 3 —NR 10 —SO 2 -phenyl; R 10 is independently selected at each occurrence from —H and —C 1-3 alkyl; and R 12 is selected from (b) measuring the amount of detectably labeled substituted 2-azetidinone glucuronide compound that is bound to NPC1L1, wherein binding of said candidate compound to human NPC1L1 decreases binding of said detectably labeled substituted 2-azetidinone glucuronide to human NPC1L1, and indicates that the candidate compound is a ligand of human NPC1L1.