Reaction Details Report a problem with these data
Target
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha/beta
Ligand
BDBM528347
Substrate
n/a
Meas. Tech.
PDE Enzyme Assays Using [3H]cGMP as Substrate
IC50
>10000±n/a nM
Citation
 Genin, MJ; Holloway, WG; Johnston, RD; Morphy, JR; Shi, Q [1,2,4]Triazolo[4,3-A]pyrazin-6(5H)-one derivatives US Patent  US11180503 Publication Date 11/23/2021 
Target
Name:
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha/beta
Synonyms:
PDE 6AB | PDE6AB | Rod cGMP-specific 3'''''''',5''''''''-cyclic phosphodiesterase alpha/beta | Rod cGMP-specific 3'''',5''''-cyclic phosphodiesterase alpha/beta | Rod cGMP-specific 3'',5''-cyclic phosphodiesterase alpha/beta | Rod cGMP-specific 3',5'-cyclic phosphodiesterase alpha/beta
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 2 components.
Component 1
Name:
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit alpha
Synonyms:
PDE6A | PDE6A_HUMAN | PDEA | Rod cGMP-specific 3',5'-cyclic phosphodiesterase alpha
Type:
PROTEIN
Mol. Mass.:
99531.10
Organism:
Human
Description:
ChEMBL_1347866
Residue:
860
Sequence:
MGEVTAEEVEKFLDSNIGFAKQYYNLHYRAKLISDLLGAKEAAVDFSNYHSPSSMEESEIIFDLLRDFQENLQTEKCIFNVMKKLCFLLQADRMSLFMYRTRNGIAELATRLFNVHKDAVLEDCLVMPDQEIVFPLDMGIVGHVAHSKKIANVPNTEEDEHFCDFVDILTEYKTKNILASPIMNGKDVVAIIMAVNKVDGSHFTKRDEEILLKYLNFANLIMKVYHLSYLHNCETRRGQILLWSGSKVFEELTDIERQFHKALYTVRAFLNCDRYSVGLLDMTKQKEFFDVWPVLMGEVPPYSGPRTPDGREINFYKVIDYILHGKEDIKVIPNPPPDHWALVSGLPAYVAQNGLICNIMNAPAEDFFAFQKEPLDESGWMIKNVLSMPIVNKKEEIVGVATFYNRKDGKPFDEMDETLMESLTQFLGWSVLNPDTYESMNKLENRKDIFQDIVKYHVKCDNEEIQKILKTREVYGKEPWECEEEELAEILQAELPDADKYEINKFHFSDLPLTELELVKCGIQMYYELKVVDKFHIPQEALVRFMYSLSKGYRKITYHNWRHGFNVGQTMFSLLVTGKLKRYFTDLEALAMVTAAFCHDIDHRGTNNLYQMKSQNPLAKLHGSSILERHHLEFGKTLLRDESLNIFQNLNRRQHEHAIHMMDIAIIATDLALYFKKRTMFQKIVDQSKTYESEQEWTQYMMLEQTRKEIVMAMMMTACDLSAITKPWEVQSQVALLVAAEFWEQGDLERTVLQQNPIPMMDRNKADELPKLQVGFIDFVCTFVYKEFSRFHEEITPMLDGITNNRKEWKALADEYDAKMKVQEEKKQKQQSAKSAAAGNQPGGNPSPGGATTSKSCCIQ
  
Component 2
Name:
Rod cGMP-specific 3',5'-cyclic phosphodiesterase subunit beta
Synonyms:
GMP-PDE beta | PDE6B | PDE6B_HUMAN | PDEB
Type:
PROTEIN
Mol. Mass.:
98308.48
Organism:
Human
Description:
ChEMBL_105761
Residue:
854
Sequence:
MSLSEEQARSFLDQNPDFARQYFGKKLSPENVAAACEDGCPPDCDSLRDLCQVEESTALLELVQDMQESINMERVVFKVLRRLCTLLQADRCSLFMYRQRNGVAELATRLFSVQPDSVLEDCLVPPDSEIVFPLDIGVVGHVAQTKKMVNVEDVAECPHFSSFADELTDYKTKNMLATPIMNGKDVVAVIMAVNKLNGPFFTSEDEDVFLKYLNFATLYLKIYHLSYLHNCETRRGQVLLWSANKVFEELTDIERQFHKAFYTVRAYLNCERYSVGLLDMTKEKEFFDVWSVLMGESQPYSGPRTPDGREIVFYKVIDYVLHGKEEIKVIPTPSADHWALASGLPSYVAESGFICNIMNASADEMFKFQEGALDDSGWLIKNVLSMPIVNKKEEIVGVATFYNRKDGKPFDEQDEVLMESLTQFLGWSVMNTDTYDKMNKLENRKDIAQDMVLYHVKCDRDEIQLILPTRARLGKEPADCDEDELGEILKEELPGPTTFDIYEFHFSDLECTELDLVKCGIQMYYELGVVRKFQIPQEVLVRFLFSISKGYRRITYHNWRHGFNVAQTMFTLLMTGKLKSYYTDLEAFAMVTAGLCHDIDHRGTNNLYQMKSQNPLAKLHGSSILERHHLEFGKFLLSEETLNIYQNLNRRQHEHVIHLMDIAIIATDLALYFKKRAMFQKIVDESKNYQDKKSWVEYLSLETTRKEIVMAMMMTACDLSAITKPWEVQSKVALLVAAEFWEQGDLERTVLDQQPIPMMDRNKAAELPKLQVGFIDFVCTFVYKEFSRFHEEILPMFDRLQNNRKEWKALADEYEAKVKALEEKEEEERVAAKKVGTEICNGGPAPKSSTCCIL
  
Inhibitor
Name:
BDBM528347
Synonyms:
9-([1,1'-bi(cylopropan)]-1-yl)-5-(cyclopropylmethyl)-2-hydroxypyrido[3,2-e][1,2,4]triazolo[4,3-a]pyrazin-6(5H)-one | US11180503, Example 5
Type:
Small organic molecule
Emp. Form.:
C18H19N5O2
Mol. Mass.:
337.3758
SMILES:
Oc1ccc2n(CC3CC3)c(=O)c3nnc(n3c2n1)C1(CC1)C1CC1
Structure:
Search PDB for entries with ligand similarity: