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Target
Glucagon-like peptide 1 receptor
Ligand
BDBM474042
Substrate
n/a
Meas. Tech.
cAMP Assay
EC50
2.30±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:
BDBM474042
Synonyms:
US10858356, Example 22
Type:
Small organic molecule
Emp. Form.:
C49H49FN10O6
Mol. Mass.:
892.9752
SMILES:
C[C@H]1C[C@]1(c1noc(=O)[nH]1)n1c(cc2cc(ccc12)C1CCOCC1)C(=O)N1CCc2nn(c(c2[C@@H]1C)-n1ccn(-c2ccc3n(ncc3c2)C2CCOC2)c1=O)-c1cc(C)c(F)c(C)c1 |r,wU:1.0,wD:35.42,3.11,(-7.89,-7.23,;-7.12,-5.9,;-7.12,-4.36,;-5.79,-5.13,;-5.47,-6.64,;-6.5,-7.78,;-5.73,-9.11,;-4.22,-8.79,;-3.08,-9.82,;-4.06,-7.26,;-4.65,-4.1,;-4.81,-2.57,;-3.4,-1.94,;-2.37,-3.09,;-.83,-3.09,;-.06,-4.42,;-.83,-5.75,;-2.37,-5.75,;-3.14,-4.42,;1.48,-4.42,;2.25,-5.75,;3.79,-5.75,;4.56,-4.42,;3.79,-3.09,;2.25,-3.09,;-6.14,-1.8,;-7.47,-2.57,;-6.14,-.26,;-7.47,.51,;-7.47,2.05,;-6.14,2.82,;-5.82,4.33,;-4.29,4.49,;-3.66,3.08,;-4.81,2.05,;-4.81,.51,;-3.47,-.26,;-2.16,2.76,;-1.76,1.28,;-.22,1.19,;.33,2.63,;1.82,3.03,;1.82,4.57,;3.15,5.34,;4.49,4.57,;5.95,5.05,;6.86,3.8,;5.95,2.55,;4.49,3.03,;3.15,2.26,;6.43,6.51,;5.52,7.76,;6.43,9,;7.89,8.53,;7.89,6.99,;-.86,3.49,;-.86,5.14,;-3.52,5.82,;-4.29,7.16,;-3.52,8.49,;-4.29,9.82,;-1.98,8.49,;-1.21,9.82,;-1.21,7.16,;.33,7.16,;-1.98,5.82,)|
Structure:
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