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ChEMBL ligand: CHEMBL10971 (SCH-37370) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
ChEMBL | Inhibitory concentration against histamine H1 receptor | B | 7 | pIC50 | 100 | nM | IC50 | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
H1 receptor/Histamine H1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390] | ||||||||
ChEMBL | Binding affinity to histamine H1 receptor in rat brain membranes was evaluated using [3H]-pyrilamine as radioligand | B | 6.49 | pKi | 320 | nM | Ki | J Med Chem (1991) 34: 457-461 [PMID:1671420] |
ChEMBL | Ability to displace [3H]-pyrilamine from H1 receptor in rat brain membrane. | B | 6.49 | pKi | 320 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 1073-1078 |
ChEMBL | Binding affinity against Histamine H1 receptor using receptor binding assay in rat brain membranes | B | 6.49 | pKi | 320 | nM | Ki | Bioorg Med Chem Lett (1998) 8: 3469-3474 [PMID:9934454] |
PAF receptor/Platelet activating factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105] | ||||||||
ChEMBL | Inhibitory concentration against platelet activating factor receptor | B | 6.08 | pIC50 | 840 | nM | IC50 | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
GtoPdb | - | - | 6.2 | pIC50 | - | - | - | Bioorg Med Chem (1999) 7: 1413-23 [PMID:10465415] |
ChEMBL | Concentration required to cause 50% inhibition of platelet activating factor (PAF)-induced platelet aggregation of human platelet rich plasma when challenged with 25 nM PAF. | F | 6.21 | pIC50 | 610 | nM | IC50 | J Med Chem (1991) 34: 457-461 [PMID:1671420] |
farnesyltransferase, CAAX box, subunit alpha/farnesyltransferase, CAAX box, subunit beta/Protein farnesyltransferase in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094108] [GtoPdb: 2825, 2826] [UniProtKB: P49354, P49356] | ||||||||
ChEMBL | Inhibitory concentration against farnesyltransferase was determined | B | 4.57 | pIC50 | 27000 | nM | IC50 | J Med Chem (2004) 47: 1869-1878 [PMID:15055985] |
B0AT2/Sodium-dependent neutral amino acid transporter B(0)AT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3351189] [GtoPdb: 940] [UniProtKB: Q9H2J7] | ||||||||
ChEMBL | Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay | B | 4.26 | pIC50 | 54800 | nM | IC50 | J Med Chem (2014) 57: 9473-9479 [PMID:25318072] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]