SCH 37370 [Ligand Id: 1853] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL10971 (SCH-37370)
  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
  • H1 receptor/Histamine H1 receptor in Rat [ChEMBL: CHEMBL4701] [GtoPdb: 262] [UniProtKB: P31390]
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  • PAF receptor/Platelet activating factor receptor in Human [ChEMBL: CHEMBL250] [GtoPdb: 334] [UniProtKB: P25105]
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  • farnesyltransferase, CAAX box, subunit alpha/farnesyltransferase, CAAX box, subunit beta/Protein farnesyltransferase in Human [ChEMBL: CHEMBL2094108] [GtoPdb: 28252826] [UniProtKB: P49354P49356]
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  • B0AT2/Sodium-dependent neutral amino acid transporter B(0)AT2 in Human [ChEMBL: CHEMBL3351189] [GtoPdb: 940] [UniProtKB: Q9H2J7]
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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: 28252826] [UniProtKB: P49354P49356]
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]