| Reaction Details |
|---|
 | Report a problem with these data |
| Target | cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A/3B |
|---|
| Ligand | BDBM14769 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_156622 (CHEMBL759867) |
|---|
| IC50 | 631±n/a nM |
|---|
| Citation |  Van der Mey, M; Bommelé, KM; Boss, H; Hatzelmann, A; Van Slingerland, M; Sterk, GJ; Timmerman, H Synthesis and structure-activity relationships of cis-tetrahydrophthalazinone/pyridazinone hybrids: a novel series of potent dual PDE3/PDE4 inhibitory agents. J Med Chem46:2008-16 (2003) [PubMed] Article |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A/3B |
|---|
| Name: | cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A/3B |
|---|
| Synonyms: | Phosphodiesterase (PDE3) | Phosphodiesterase 3 | Phosphodiesterase 3 (PDE3) | cGMP-inhibited 3',5'-cyclic phosphodiesterase A/B |
|---|
| Type: | n/a |
|---|
| Mol. Mass.: | n/a |
|---|
| Description: | ASSAY_ID of ChEMBL is 156458 |
|---|
| Components: | This complex has 2 components. |
|---|
| Component 1 |
| Name: | cGMP-inhibited 3',5'-cyclic phosphodiesterase 3B |
|---|
| Synonyms: | CGI-PDE B | CGIP1 | CGIPDE1 | Cyclic GMP-inhibited phosphodiesterase B | PDE3B | PDE3B_HUMAN | Phosphodiesterase 3B | Phosphodiesterase 3B (PDE3B) | Phosphodiesterase Type 3 (PDE3B) | cGMP-inhibited 3',5'-cyclic phosphodiesterase B | cGMP-inhibited 3,5-cyclic phosphodiesterase B |
|---|
| Type: | Enzyme |
|---|
| Mol. Mass.: | 124318.95 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | PDE3B was generated from the full-length recombinant human clone transfected into Sf9 cells. |
|---|
| Residue: | 1112 |
|---|
| Sequence: | MRRDERDAKAMRSLQPPDGAGSPPESLRNGYVKSCVSPLRQDPPRGFFFHLCRFCNVELR
PPPASPQQPRRCSPFCRARLSLGALAAFVLALLLGAEPESWAAGAAWLRTLLSVCSHSLS
PLFSIACAFFFLTCFLTRTKRGPGPGRSCGSWWLLALPACCYLGDFLVWQWWSWPWGDGD
AGSAAPHTPPEAAAGRLLLVLSCVGLLLTLAHPLRLRHCVLVLLLASFVWWVSFTSLGSL
PSALRPLLSGLVGGAGCLLALGLDHFFQIREAPLHPRLSSAAEEKVPVIRPRRRSSCVSL
GETAASYYGSCKIFRRPSLPCISREQMILWDWDLKQWYKPHYQNSGGGNGVDLSVLNEAR
NMVSDLLTDPSLPPQVISSLRSISSLMGAFSGSCRPKINPLTPFPGFYPCSEIEDPAEKG
DRKLNKGLNRNSLPTPQLRRSSGTSGLLPVEQSSRWDRNNGKRPHQEFGISSQGCYLNGP
FNSNLLTIPKQRSSSVSLTHHVGLRRAGVLSSLSPVNSSNHGPVSTGSLTNRSPIEFPDT
ADFLNKPSVILQRSLGNAPNTPDFYQQLRNSDSNLCNSCGHQMLKYVSTSESDGTDCCSG
KSGEEENIFSKESFKLMETQQEEETEKKDSRKLFQEGDKWLTEEAQSEQQTNIEQEVSLD
LILVEEYDSLIEKMSNWNFPIFELVEKMGEKSGRILSQVMYTLFQDTGLLEIFKIPTQQF
MNYFRALENGYRDIPYHNRIHATDVLHAVWYLTTRPVPGLQQIHNGCGTGNETDSDGRIN
HGRIAYISSKSCSNPDESYGCLSSNIPALELMALYVAAAMHDYDHPGRTNAFLVATNAPQ
AVLYNDRSVLENHHAASAWNLYLSRPEYNFLLHLDHVEFKRFRFLVIEAILATDLKKHFD
FLAEFNAKANDVNSNGIEWSNENDRLLVCQVCIKLADINGPAKVRDLHLKWTEGIVNEFY
EQGDEEANLGLPISPFMDRSSPQLAKLQESFITHIVGPLCNSYDAAGLLPGQWLEAEEDN
DTESGDDEDGEELDTEDEEMENNLNPKPPRRKSRRRIFCQLMHHLTENHKIWKEIVEEEE
KCKADGNKLQVENSSLPQADEIQVIEEADEEE
|
|
|
|---|
| Component 2 |
| Name: | cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A |
|---|
| Synonyms: | 3',5'-cyclic phosphodiesterase | CGI-PDE A | Cyclic GMP-inhibited phosphodiesterase A | PDE3A | PDE3A_HUMAN | Phosphodiesterase 3 | Phosphodiesterase 3 (PDE3) | Phosphodiesterase 3 and 5 (PDE3 and PDE5) | Phosphodiesterase 3A | Phosphodiesterase 3A (PDE3A) | Phosphodiesterase 3A (PDE3A1) | Phosphodiesterase Type 3 (PDE3A) | cGMP-inhibited 3',5'-cyclic phosphodiesterase A | cGMP-inhibited 3,5-cyclic phosphodiesterase A |
|---|
| Type: | Enzyme |
|---|
| Mol. Mass.: | 124966.46 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | Q14432 |
|---|
| Residue: | 1141 |
|---|
| Sequence: | MAVPGDAARVRDKPVHSGVSQAPTAGRDCHHRADPASPRDSGCRGCWGDLVLQPLRSSRK
LSSALCAGSLSFLLALLVRLVRGEVGCDLEQCKEAAAAEEEEAAPGAEGGVFPGPRGGAP
GGGARLSPWLQPSALLFSLLCAFFWMGLYLLRAGVRLPLAVALLAACCGGEALVQIGLGV
GEDHLLSLPAAGVVLSCLAAATWLVLRLRLGVLMIALTSAVRTVSLISLERFKVAWRPYL
AYLAGVLGILLARYVEQILPQSAEAAPREHLGSQLIAGTKEDIPVFKRRRRSSSVVSAEM
SGCSSKSHRRTSLPCIPREQLMGHSEWDHKRGPRGSQSSGTSITVDIAVMGEAHGLITDL
LADPSLPPNVCTSLRAVSNLLSTQLTFQAIHKPRVNPVTSLSENYTCSDSEESSEKDKLA
IPKRLRRSLPPGLLRRVSSTWTTTTSATGLPTLEPAPVRRDRSTSIKLQEAPSSSPDSWN
NPVMMTLTKSRSFTSSYAISAANHVKAKKQSRPGALAKISPLSSPCSSPLQGTPASSLVS
KISAVQFPESADTTAKQSLGSHRALTYTQSAPDLSPQILTPPVICSSCGRPYSQGNPADE
PLERSGVATRTPSRTDDTAQVTSDYETNNNSDSSDIVQNEDETECLREPLRKASACSTYA
PETMMFLDKPILAPEPLVMDNLDSIMEQLNTWNFPIFDLVENIGRKCGRILSQVSYRLFE
DMGLFEAFKIPIREFMNYFHALEIGYRDIPYHNRIHATDVLHAVWYLTTQPIPGLSTVIN
DHGSTSDSDSDSGFTHGHMGYVFSKTYNVTDDKYGCLSGNIPALELMALYVAAAMHDYDH
PGRTNAFLVATSAPQAVLYNDRSVLENHHAAAAWNLFMSRPEYNFLINLDHVEFKHFRFL
VIEAILATDLKKHFDFVAKFNGKVNDDVGIDWTNENDRLLVCQMCIKLADINGPAKCKEL
HLQWTDGIVNEFYEQGDEEASLGLPISPFMDRSAPQLANLQESFISHIVGPLCNSYDSAG
LMPGKWVEDSDESGDTDDPEEEEEEAPAPNEEETCENNESPKKKTFKRRKIYCQITQHLL
QNHKMWKKVIEEEQRLAGIENQSLDQTPQSHSSEQIQAIKEEEEEKGKPRGEEIPTQKPD
Q
|
|
|
|---|
| BDBM14769 |
|---|
| n/a |
|---|
| Name | BDBM14769 |
|---|
| Synonyms: | 6-(3,4-Dimethoxy-phenyl)-4,5-dimethyl-4,5-dihydro-2H-pyridazin-3-one | 6-(4-(difluoromethoxy)-3-methoxyphenyl)pyridazin-3(2H)-one | 6-(4-Difluoromethoxy-3-methoxy-phenyl)-2H-pyridazin-3-one | 6-[4-(difluoromethoxy)-3-methoxyphenyl]-2,3-dihydropyridazin-3-one | CHEMBL313842 | Zaradaverine | Zardaverine |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C12H10F2N2O3 |
|---|
| Mol. Mass. | 268.2162 |
|---|
| SMILES | COc1cc(ccc1OC(F)F)-c1ccc(=O)[nH]n1 |
|---|
| Structure | 
|
|---|
Search and Browse
