[3H]tiotidine [Ligand Id: 3959] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL269646 (ICI 125,211, ICI-125,211, ICI-125211, Tiotidina, Tiotidine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
| GtoPdb | - | - | 8.7 | pKd | 2.2 | nM | Kd | Mol Pharmacol (2003) 64: 512-20 [PMID:12869657] |
| ChEMBL | Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| ChEMBL | Displacement of [125I]Aminopotentidine from human recombinant histamine H2 receptor expressed in CHOK1 cells after 2 hrs | B | 7.66 | pIC50 | 22 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 1834-1838 [PMID:23403082] |
| Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747] | ||||||||
| ChEMBL | Evaluated in vitro for Histamine H2 receptor inhibition using the dimaprit stimulated chronotropic response of the guinea pig atrium | B | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (1983) 26: 140-144 [PMID:6131129] |
| ChEMBL | Inhibition of [125I]APT binding to H2 receptors in guinea pig cerebral membranes. | B | 8.25 | pKi | 5.62 | nM | Ki | J Med Chem (1992) 35: 2231-2238 [PMID:1613748] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBCs by firefly luciferase reporter gene assay | F | 4.64 | pIC50 | >22750 | nM | IC50 | Antimicrob Agents Chemother (2010) 54: 3597-3604 [PMID:20547797] |
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]
