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Target
Glucagon-like peptide 1 receptor
Ligand
BDBM474067
Substrate
n/a
Meas. Tech.
cAMP Assay
EC50
2.00±n/a nM
Citation
 Yoshino, H; Tsuchiya, S; Matsuo, A; Sato, T; Nishimoto, M; Oguri, K; Ogawa, H; Nishimura, Y; Furuta, Y; Kashiwagi, H; Hori, N; Kamon, T; Shiraishi, T; Yoshida, S; Kawai, T; Tanida, S; Aoki, M Pyrazolopyridine derivative having GLP-1 receptor agonist effect US Patent  US10858356 Publication Date 12/8/2020 
Target
Name:
Glucagon-like peptide 1 receptor
Synonyms:
GLP-1 receptor | GLP-1-R | GLP-1R | GLP1R | GLP1R_HUMAN | Glucagon-like peptide 1 receptor | Glucagon-like peptide 1 receptor (GLP-1)
Type:
Enzyme
Mol. Mass.:
53035.78
Organism:
Homo sapiens (Human)
Description:
P43220
Residue:
463
Sequence:
MAGAPGPLRLALLLLGMVGRAGPRPQGATVSLWETVQKWREYRRQCQRSLTEDPPPATDLFCNRTFDEYACWPDGEPGSFVNVSCPWYLPWASSVPQGHVYRFCTAEGLWLQKDNSSLPWRDLSECEESKRGERSSPEEQLLFLYIIYTVGYALSFSALVIASAILLGFRHLHCTRNYIHLNLFASFILRALSVFIKDAALKWMYSTAAQQHQWDGLLSYQDSLSCRLVFLLMQYCVAANYYWLLVEGVYLYTLLAFSVLSEQWIFRLYVSIGWGVPLLFVVPWGIVKYLYEDEGCWTRNSNMNYWLIIRLPILFAIGVNFLIFVRVICIVVSKLKANLMCKTDIKCRLAKSTLTLIPLLGTHEVIFAFVMDEHARGTLRFIKLFTELSFTSFQGLMVAILYCFVNNEVQLEFRKSWERWRLEHLHIQRDSSMKPLKCPTSSLSSGATAGSSMYTATCQASCS
  
Inhibitor
Name:
BDBM474067
Synonyms:
US10858356, Example 47
Type:
Small organic molecule
Emp. Form.:
C47H46F2N10O6
Mol. Mass.:
884.9283
SMILES:
COCCn1ncc2c(F)c(ccc12)-n1ccn(-c2c3[C@H](C)N(CCc3nn2-c2ccc(F)c(C)c2)C(=O)c2cc3cc(ccc3n2[C@]2(C[C@@H]2C)c2noc(=O)[nH]2)C2CCOCC2)c1=O |r,wU:49.57,wD:20.22,47.53,(8.83,9.12,;7.32,8.8,;6.85,7.33,;5.34,7.01,;4.87,5.55,;5.77,4.3,;4.87,3.06,;3.4,3.53,;2.07,2.76,;2.07,1.22,;.73,3.53,;.73,5.07,;2.07,5.84,;3.4,5.07,;-.6,2.76,;-1.08,1.3,;-2.62,1.3,;-3.09,2.76,;-4.6,3.08,;-5.74,2.05,;-5.74,.51,;-4.41,-.26,;-7.08,-.26,;-8.41,.51,;-8.41,2.05,;-7.08,2.82,;-6.76,4.33,;-5.22,4.49,;-4.45,5.82,;-2.91,5.82,;-2.14,7.16,;-2.91,8.49,;-2.14,9.82,;-4.45,8.49,;-5.22,9.82,;-5.22,7.16,;-7.08,-1.8,;-8.41,-2.57,;-5.74,-2.57,;-4.34,-1.94,;-3.31,-3.09,;-1.77,-3.09,;-1,-4.42,;-1.77,-5.75,;-3.31,-5.75,;-4.08,-4.42,;-5.58,-4.1,;-6.73,-5.13,;-8.06,-4.36,;-8.06,-5.9,;-8.83,-7.23,;-6.41,-6.64,;-7.44,-7.78,;-6.67,-9.11,;-5.16,-8.79,;-4.02,-9.82,;-5,-7.26,;.54,-4.42,;1.31,-5.75,;2.85,-5.75,;3.62,-4.42,;2.85,-3.09,;1.31,-3.09,;-1.85,3.67,;-1.85,5.21,)|
Structure:
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