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TargetP2X purinoceptor 7
LigandBDBM254203
Substrate/Competitorn/a
Meas. Tech.ChEMBL_1703525 (CHEMBL4054758)
Ki 2.2±n/a nM
Citation Letavic, MASavall, BMAllison, BDAluisio, LAndres, JIDe Angelis, MAo, HBeauchamp, DABonaventure, PBryant, SCarruthers, NICeusters, MCoe, KJDvorak, CAFraser, ICGelin, CFKoudriakova, TLiang, JLord, BLovenberg, TWOtieno, MASchoetens, FSwanson, DMWang, QWickenden, ADBhattacharya, A 4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate. J Med Chem60:4559-4572 (2017) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
P2X purinoceptor 7
Name:P2X purinoceptor 7
Synonyms:ATP receptor | P2RX7_RAT | P2X purinoceptor 7 | P2X purinoceptor 7 (P2RX7) | P2X purinoceptor 7 (P2X7) | P2X7 | P2X7 rat | P2Z receptor | P2rx7 | Purinergic receptor
Type:Protein
Mol. Mass.:68403.50
Organism:Rattus norvegicus (Rat)
Description:Q64663
Residue:595
Sequence:
MPACCSWNDVFQYETNKVTRIQSVNYGTIKWILHMTVFSYVSFALMSDKLYQRKEPLISS
VHTKVKGVAEVTENVTEGGVTKLVHGIFDTADYTLPLQGNSFFVMTNYLKSEGQEQKLCP
EYPSRGKQCHSDQGCIKGWMDPQSKGIQTGRCIPYDQKRKTCEIFAWCPAEEGKEAPRPA
LLRSAENFTVLIKNNIDFPGHNYTTRNILPGMNISCTFHKTWNPQCPIFRLGDIFQEIGE
NFTEVAVQGGIMGIEIYWDCNLDSWSHRCQPKYSFRRLDDKYTNESLFPGYNFRYAKYYK
ENGMEKRTLIKAFGVRFDILVFGTGGKFDIIQLVVYIGSTLSYFGLATVCIDLIINTYAS
TCCRSRVYPSCKCCEPCAVNEYYYRKKCEPIVEPKPTLKYVSFVDEPHIWMVDQQLLGKS
LQDVKGQEVPRPQTDFLELSRLSLSLHHSPPIPGQPEEMQLLQIEAVPRSRDSPDWCQCG
NCLPSQLPENRRALEELCCRRKPGQCITTSELFSKIVLSREALQLLLLYQEPLLALEGEA
INSKLRHCAYRSYATWRFVSQDMADFAILPSCCRWKIRKEFPKTQGQYSGFKYPY
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  Blast E-value cutoff:
BDBM254203
n/a
NameBDBM254203
Synonyms:US10112937, Example 88 | US10150765, Example 88 | US10703749, Example 88 | US9464084, 88
TypeSmall organic molecule
Emp. Form.C18H14ClF3N6O
Mol. Mass.422.792
SMILESC[C@H]1N(CCc2c1nnn2-c1ncccn1)C(=O)c1cccc(c1Cl)C(F)(F)F |r|
Structure
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