Reaction Details |
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Target | Tryptase beta-2/delta/gamma |
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Ligand | BDBM50120387 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_210690 (CHEMBL817288) |
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IC50 | <1.7±n/a nM |
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Citation | Bisacchi, GS; Slusarchyk, WA; Bolton, SA; Hartl, KS; Jacobs, G; Mathur, A; Meng, W; Ogletree, ML; Pi, Z; Sutton, JC; Treuner, U; Zahler, R; Zhao, G; Seiler, SM Synthesis of potent and highly selective nonguanidine azetidinone inhibitors of human tryptase. Bioorg Med Chem Lett14:2227-31 (2004) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Tryptase beta-2/delta/gamma |
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Name: | Tryptase beta-2/delta/gamma |
Synonyms: | Tryptase |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 1510505 |
Components: | This complex has 3 components. |
Component 1 |
Name: | Tryptase gamma |
Synonyms: | PRSS31 | Serine protease 31 | TMT | TPSG1 | TRYG1_HUMAN | Transmembrane tryptase | Tryptase | Tryptase gamma | Tryptase gamma heavy chain | Tryptase gamma light chain |
Type: | PROTEIN |
Mol. Mass.: | 33817.52 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_210833 |
Residue: | 321 |
Sequence: | MALGACGLLLLLAVPGVSLRTLQPGCGRPQVSDAGGRIVGGHAAPAGAWPWQASLRLRRM
HVCGGSLLSPQWVLTAAHCFSGSLNSSDYQVHLGELEITLSPHFSTVRQIILHSSPSGQP
GTSGDIALVELSVPVTLSSRILPVCLPEASDDFCPGIRCWVTGWGYTREGEPLPPPYSLR
EVKVSVVDTETCRRDYPGPGGSILQPDMLCARGPGDACQDDSGGPLVCQVNGAWVQAGTV
SWGEGCGRPNRPGVYTRVPAYVNWIRRHITASGGSESGYPRLPLLAGLFLPGLFLLLVSC
VLLAKCLLHPSADGTPFPAPD
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Component 2 |
Name: | Tryptase beta-2 |
Synonyms: | TPS2 | TPSB2 | TRYB2_HUMAN | Tryptase | Tryptase II | Tryptase beta-1 | Tryptase-2 |
Type: | PROTEIN |
Mol. Mass.: | 30518.79 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_210702 |
Residue: | 275 |
Sequence: | MLNLLLLALPVLASRAYAAPAPGQALQRVGIVGGQEAPRSKWPWQVSLRVHGPYWMHFCG
GSLIHPQWVLTAAHCVGPDVKDLAALRVQLREQHLYYQDQLLPVSRIIVHPQFYTAQIGA
DIALLELEEPVNVSSHVHTVTLPPASETFPPGMPCWVTGWGDVDNDERLPPPFPLKQVKV
PIMENHICDAKYHLGAYTGDDVRIVRDDMLCAGNTRRDSCQGDSGGPLVCKVNGTWLQAG
VVSWGEGCAQPNRPGIYTRVTYYLDWIHHYVPKKP
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Component 3 |
Name: | Tryptase delta |
Synonyms: | Delta-tryptase | HmMCP-3-like tryptase III | Mast cell mMCP-7-like | TPSD1 | TRYD_HUMAN | Tryptase delta | Tryptase-3 |
Type: | PROTEIN |
Mol. Mass.: | 26578.73 |
Organism: | Homo sapiens (Human) |
Description: | ChEMBL_104777 |
Residue: | 242 |
Sequence: | MLLLAPQMLSLLLLALPVLASPAYVAPAPGQALQQTGIVGGQEAPRSKWPWQVSLRVRGP
YWMHFCGGSLIHPQWVLTAAHCVEPDIKDLAALRVQLREQHLYYQDQLLPVSRIIVHPQF
YIIQTGADIALLELEEPVNISSHIHTVTLPPASETFPPGMPCWVTGWGDVDNNVHLPPPY
PLKEVEVPVVENHLCNAEYHTGLHTGHSFQIVRDDMLCAGSENHDSCQGDSGGPLVCKVN
GT
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BDBM50120387 |
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n/a |
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Name | BDBM50120387 |
Synonyms: | (2S,3R)-3-((R)-1-Carbamimidoyl-piperidin-3-ylmethyl)-4-oxo-1-[4-(6-phenyl-hexanoyl)-piperazine-1-carbonyl]-azetidine-2-carboxylic acid | (2S,3R)-3-(1-Carbamimidoyl-piperidin-3-ylmethyl)-4-oxo-1-[4-((R)-6-phenyl-hexanoyl)-piperazine-1-carbonyl]-azetidine-2-carboxylic acid | (2S,3R)-3-(1-Carbamimidoyl-piperidin-3-ylmethyl)-4-oxo-1-[4-(5-phenyl-pentanoyl)-piperazine-1-carbonyl]-azetidine-2-carboxylic acid | BMS-363131 | CHEMBL303437 |
Type | Small organic molecule |
Emp. Form. | C28H40N6O5 |
Mol. Mass. | 540.6544 |
SMILES | NC(=N)N1CCC[C@H](C[C@@H]2[C@H](N(C(=O)N3CCN(CC3)C(=O)CCCCCc3ccccc3)C2=O)C(O)=O)C1 |
Structure |
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