Ki Summary

Reaction Details

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Target

Bifunctional dihydrofolate reductase-thymidylate synthase [1-238,S58R,S117N]

Ligand

BDBM18791

Substrate/Competitor

BDBM18044

Meas. Tech.

Inhibitor Screening Using Bacterial System (IC50) and Measurement of Inhibition Constant (Ki)

0.81±n/a nM

IC50

2760±n/a nM

Citation

Bunyarataphan, S; Leartsakulpanich, U; Taweechai, S; Tarnchompoo, B; Kamchonwongpaisan, S; Yuthavong, Y Evaluation of the activities of pyrimethamine analogs against Plasmodium vivax and Plasmodium falciparum dihydrofolate reductase-thymidylate synthase using in vitro enzyme inhibition and bacterial complementation assays. Antimicrob Agents Chemother50:3631-7 (2006) [PubMed] Article

More Info.:

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

Bifunctional dihydrofolate reductase-thymidylate synthase [1-238,S58R,S117N]

Name:

Bifunctional dihydrofolate reductase-thymidylate synthase [1-238,S58R,S117N]

Synonyms:

DRTS_PLAVI | Dihydrofolate Reductase-Thymidylate Synthase (DHFR-TS) Muatnt (S58R/S117N) | Dihydrofolate Reductase-Thymidylate Synthase (DHFR-TS) Mutant SP21

Type:

Enzyme

Mol. Mass.:

27235.37

Organism:

Plasmodium vivax (malaria parasite P. vivax)

Description:

O02604[1-238,S58R,S117N]

Residue:

238

Sequence:

MENLSDVFDIYAICACCKVAPTSEGTKNEPFSPRTFRGLGNKGTLPWKCNSVDMKYFRSV
TTYVDESKYEKLKWKRERYLRMEASQGGGDNTSGGDNTHGGDNADKLQNVVVMGRSNWES
IPKQYKPLPNRINVVLSKTLTKEDVKEKVFIIDSIDDLLLLLKKLKYYKCFIIGGAQVYR
ECLSRNLIKQIYFTRINGAYPCDVFFPEFDESEFRVTSVSEVYNSKGTTLDFLVYSKV

BDBM18791

BDBM18044

Name

BDBM18791

Synonyms:

5-phenyl-6-(3-phenylpropyl)pyrimidine-2,4-diamine | CHEMBL22693 | P33

Type

Small organic molecule

Emp. Form.

C19H20N4

Mol. Mass.

304.3889

SMILES

Nc1nc(N)c(-c2ccccc2)c(CCCc2ccccc2)n1

Structure