Reaction Details |
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Target | Lysosomal acid glucosylceramidase |
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Ligand | BDBM18449 |
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Substrate/Competitor | BDBM18429 |
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Meas. Tech. | GC Enzyme Assay |
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pH | 5.9±n/a |
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Temperature | 294.15±n/a K |
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Ki | 4230±n/a nM |
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IC50 | 7730±n/a nM |
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Km | 28000±n/a nM |
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Citation | Zheng, W; Padia, J; Urban, DJ; Jadhav, A; Goker-Alpan, O; Simeonov, A; Goldin, E; Auld, D; LaMarca, ME; Inglese, J; Austin, CP; Sidransky, E Three classes of glucocerebrosidase inhibitors identified by quantitative high-throughput screening are chaperone leads for Gaucher disease. Proc Natl Acad Sci U S A104:13192-7 (2007) [PubMed] Article |
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More Info.: | Get all data from this article, Inhibition_Run data, Solution Info, Assay Method |
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Lysosomal acid glucosylceramidase |
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Name: | Lysosomal acid glucosylceramidase |
Synonyms: | Acid beta-glucosidase | Alglucerase | Beta-glucocerebrosidase | Beta-glucocerebrosidase (GC) | D-glucosyl-N-acylsphingosine glucohydrolase | GBA | GBA1 | GBA1_HUMAN | GC | GCase | GLUC | Glucocerebrosidase (GBA) | Glucosylceramidase (GBA) | Glucosylceramidase (GCase) | Glucosylceramidase precursor (Beta-glucocerebrosidase) (Acid beta-glucosidase) (D-glucosyl-N-acylsphingosine glucohydrolase) (Alglucerase) (Imiglucerase) | Imiglucerase | beta-glucocerebrosidase (GCase) |
Type: | Enzyme |
Mol. Mass.: | 59724.64 |
Organism: | Homo sapiens (Human) |
Description: | The beta-Glu activity was measured with commercially available beta-glucocerebrosidase (Ceredase) as the enzyme source. |
Residue: | 536 |
Sequence: | MEFSSPSREECPKPLSRVSIMAGSLTGLLLLQAVSWASGARPCIPKSFGYSSVVCVCNAT
YCDSFDPPTFPALGTFSRYESTRSGRRMELSMGPIQANHTGTGLLLTLQPEQKFQKVKGF
GGAMTDAAALNILALSPPAQNLLLKSYFSEEGIGYNIIRVPMASCDFSIRTYTYADTPDD
FQLHNFSLPEEDTKLKIPLIHRALQLAQRPVSLLASPWTSPTWLKTNGAVNGKGSLKGQP
GDIYHQTWARYFVKFLDAYAEHKLQFWAVTAENEPSAGLLSGYPFQCLGFTPEHQRDFIA
RDLGPTLANSTHHNVRLLMLDDQRLLLPHWAKVVLTDPEAAKYVHGIAVHWYLDFLAPAK
ATLGETHRLFPNTMLFASEACVGSKFWEQSVRLGSWDRGMQYSHSIITNLLYHVVGWTDW
NLALNPEGGPNWVRNFVDSPIIVDITKDTFYKQPMFYHLGHFSKFIPEGSQRVGLVASQK
NDLDAVALMHPDGSAVVVVLNRSSKDVPLTIKDPAVGFLETISPGYSIHTYLWRRQ
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BDBM18449 |
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BDBM18429 |
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Name | BDBM18449 |
Synonyms: | 2-({4-[(4-chlorophenyl)amino]-6-(pyrrolidin-1-yl)-1,3,5-triazin-2-yl}amino)ethan-1-ol | Triazine compound, 28 | triazine scaffold, 30 |
Type | Small organic molecule |
Emp. Form. | C15H19ClN6O |
Mol. Mass. | 334.804 |
SMILES | OCCNc1nc(Nc2ccc(Cl)cc2)nc(n1)N1CCCC1 |
Structure |
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