Ki Summary

Reaction Details

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Target

Purine nucleoside phosphorylase

Ligand

BDBM22109

Substrate/Competitor

BDBM22104

Meas. Tech.

PNP Inhibition Assay

7.7±n/a

Temperature

295.15±n/a K

1.0±0.2 nM

34000±n/a nM

Comments

Ki is the dissociation constant for the first step in the two-step binding characteristic of slow-onset tight-binding inhibition.

Citation

Evans, GB; Furneaux, RH; Greatrex, B; Murkin, AS; Schramm, VL; Tyler, PC Azetidine based transition state analogue inhibitors of N-ribosyl hydrolases and phosphorylases. J Med Chem51:948-56 (2008) [PubMed] Article

More Info.:

Get all data from this article, Solution Info, Assay Method

Purine nucleoside phosphorylase

Name:

Purine nucleoside phosphorylase

Synonyms:

Type:

Enzyme

Mol. Mass.:

32035.18

Organism:

Bos taurus (bovine)

Description:

n/a

Residue:

289

Sequence:

MANGYTYEDYQDTAKWLLSHTEQRPQVAVICGSGLGGLVNKLTQAQTFDYSEIPNFPEST
VPGHAGRLVFGILNGRACVMMQGRFHMYEGYPFWKVTFPVRVFRLLGVETLVVTNAAGGL
NPNFEVGDIMLIRDHINLPGFSGENPLRGPNEERFGVRFPAMSDAYDRDMRQKAHSTWKQ
MGEQRELQEGTYVMLGGPNFETVAECRLLRNLGADAVGMSTVPEVIVARHCGLRVFGFSL
ITNKVIMDYESQGKANHEEVLEAGKQAAQKLEQFVSLLMASIPVSGHTG

BDBM22109

BDBM22104

Name

BDBM22109

Synonyms:

7-{[(3R,4R)-3-hydroxy-4-(hydroxymethyl)pyrrolidin-1-yl]methyl}-1,5-dihydro-4H-pyrrolo[3,2-d]pyrimidin-4-one | 7-{[(3R,4R)-3-hydroxy-4-(hydroxymethyl)pyrrolidin-1-yl]methyl}-1H,4H,5H-pyrrolo[3,2-d]pyrimidin-4-one | CHEMBL1213653 | CHEMBL269864 | DADMe-ImmH,7

Type

n/a

Emp. Form.

C12H16N4O3

Mol. Mass.

264.2804

SMILES

OC[C@H]1CN(Cc2c[nH]c3c2nc[nH]c3=O)C[C@@H]1O |r|

Structure