Reaction Details |
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Target | P2X purinoceptor 7 |
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Ligand | BDBM254314 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_1683148 |
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IC50 | 7.3±n/a nM |
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Citation | Chrovian, CC; Soyode-Johnson, A; Peterson, AA; Gelin, CF; Deng, X; Dvorak, CA; Carruthers, NI; Lord, B; Fraser, I; Aluisio, L; Coe, KJ; Scott, B; Koudriakova, T; Schoetens, F; Sepassi, K; Gallacher, DJ; Bhattacharya, A; Letavic, MA A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate. J Med Chem61:207-223 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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P2X purinoceptor 7 |
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Name: | P2X purinoceptor 7 |
Synonyms: | ATP receptor | P2RX7 | P2RX7_HUMAN | P2X purinoceptor 7 (P2RX7) | P2X purinoceptor 7 (P2X7) | P2X7 | P2Z receptor | Purinergic receptor |
Type: | Protein |
Mol. Mass.: | 68602.85 |
Organism: | Homo sapiens (Human) |
Description: | Q99572 |
Residue: | 595 |
Sequence: | MPACCSCSDVFQYETNKVTRIQSMNYGTIKWFFHVIIFSYVCFALVSDKLYQRKEPVISS
VHTKVKGIAEVKEEIVENGVKKLVHSVFDTADYTFPLQGNSFFVMTNFLKTEGQEQRLCP
EYPTRRTLCSSDRGCKKGWMDPQSKGIQTGRCVVYEGNQKTCEVSAWCPIEAVEEAPRPA
LLNSAENFTVLIKNNIDFPGHNYTTRNILPGLNITCTFHKTQNPQCPIFRLGDIFRETGD
NFSDVAIQGGIMGIEIYWDCNLDRWFHHCRPKYSFRRLDDKTTNVSLYPGYNFRYAKYYK
ENNVEKRTLIKVFGIRFDILVFGTGGKFDIIQLVVYIGSTLSYFGLAAVFIDFLIDTYSS
NCCRSHIYPWCKCCQPCVVNEYYYRKKCESIVEPKPTLKYVSFVDESHIRMVNQQLLGRS
LQDVKGQEVPRPAMDFTDLSRLPLALHDTPPIPGQPEEIQLLRKEATPRSRDSPVWCQCG
SCLPSQLPESHRCLEELCCRKKPGACITTSELFRKLVLSRHVLQFLLLYQEPLLALDVDS
TNSRLRHCAYRCYATWRFGSQDMADFAILPSCCRWRIRKEFPKSEGQYSGFKSPY
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BDBM254314 |
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n/a |
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Name | BDBM254314 |
Synonyms: | US10112937, Example 212 | US10150765, Example 212 | US10703749, Example 212 | US9464084, 212 |
Type | Small organic molecule |
Emp. Form. | C18H14ClF3N6O |
Mol. Mass. | 422.792 |
SMILES | C[C@H]1Cc2c(CN1C(=O)c1cccc(c1Cl)C(F)(F)F)nnn2-c1cnccn1 |r| |
Structure |
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