Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL10971 (SCH-37370) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]