famotidine [Ligand Id: 7074] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL902 (Amfamox, Fadul, Famodil, Famosan, Famotidine, Famotidine preservative free, Famotidine preservative free (pharmacy bulk), Famoxal, Fluxid, Ganor, Gastridin, Gastropen, L 643341, Lecedil, MK-208, Motiax, Muclox, NSC-757810, Pepcid, Pepcid ac, Pepcidac, Pepcid preservative free, Pepcid rpd, Pepdine, Pepdul, YM-11170) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915] | ||||||||
| ChEMBL | Inhibition of recombinant human CA1 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 6.04 | pKi | 922.4 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | Inhibition of recombinant human CA2 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 7.24 | pKi | 57.9 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| Carbonic anhydrase III in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2885] [UniProtKB: P07451] | ||||||||
| ChEMBL | Inhibition of recombinant human CA3 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 5 | pKi | >10000 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| carbonic anhydrase 4/Carbonic anhydrase IV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748] | ||||||||
| ChEMBL | Inhibition of recombinant human CA4 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 6.03 | pKi | 938.8 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790] | ||||||||
| ChEMBL | Inhibition of recombinant human CA9 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 6.9 | pKi | 126.3 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| carbonic anhydrase 5A/Carbonic anhydrase VA in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218] | ||||||||
| ChEMBL | Inhibition of recombinant human CA5a preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 5.84 | pKi | 1429.5 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| Carbonic anhydrase VB in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0] | ||||||||
| ChEMBL | Inhibition of recombinant human CA5b preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 5.27 | pKi | 5328.2 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| Carbonic anhydrase VI in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3025] [UniProtKB: P23280] | ||||||||
| ChEMBL | Inhibition of recombinant human CA6 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 7.01 | pKi | 98.2 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| carbonic anhydrase 7/Carbonic anhydrase VII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166] | ||||||||
| ChEMBL | Inhibition of recombinant human CA7 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 8.52 | pKi | 3 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570] | ||||||||
| ChEMBL | Inhibition of recombinant human CA12 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 7.34 | pKi | 45.3 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| carbonic anhydrase 13/Carbonic anhydrase XIII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1] | ||||||||
| ChEMBL | Inhibition of recombinant human CA13 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 6.77 | pKi | 171.5 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| carbonic anhydrase 14/Carbonic anhydrase XIV in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7] | ||||||||
| ChEMBL | Inhibition of recombinant human CA14 preincubated for 15 mins prior to testing measured for 10 to 100 secs by phenol red based stopped-flow CO2 hydration assay | B | 6.17 | pKi | 677.2 | nM | Ki | ACS Med Chem Lett (2018) 9: 1035-1038 [PMID:30344913] |
| H2 receptor/Histamine H2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021] | ||||||||
| ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 7.39 | pKi | 41 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Histamine H2 radioligand binding (ligand: [125I] Aminopotentidine) | B | 7.38 | pIC50 | 42 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Histamine H2 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2882] [UniProtKB: P47747] | ||||||||
| ChEMBL | In vitro inhibitory activity against histamine H2-receptor in isolated Guinea pig right atria. | B | 7 | pKd | 100 | nM | Kd | J Med Chem (1992) 35: 2446-2451 [PMID:1352351] |
| ChEMBL | Histamine H2 receptor antagonistic activity on the isolated spontaneously beating guinea pig right atrium | F | 7.74 | pKd | 18.2 | nM | Kd | Bioorg Med Chem Lett (2003) 13: 1717-1720 [PMID:12729649] |
| ChEMBL | Compound was tested for H2 receptor antagonistic activity against histamine stimulated chronotropic response in isolated guinea pig right atrium | F | 6.52 | pIC50 | 300 | nM | IC50 | J Med Chem (1994) 37: 57-66 [PMID:7904648] |
| Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8] | ||||||||
| ChEMBL | Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 6.12 | pIC50 | 760 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| MATE2/Multidrug and toxin extrusion protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8] | ||||||||
| ChEMBL | Inhibition of human MATE2K-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay | B | 4.44 | pIC50 | 36200 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| 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] |
| Organic cation transporter 2/Solute carrier family 22 member 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244] | ||||||||
| ChEMBL | Inhibition of human OCT2-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.44 | pIC50 | 36100 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
| Organic cation transporter 3/Solute carrier family 22 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751] | ||||||||
| ChEMBL | Inhibition of human OCT3-mediated ASP+ uptake expressed in HEK293 cells after 3 mins by fluorescence assay | B | 4.97 | pIC50 | 10700 | nM | IC50 | J Med Chem (2013) 56: 781-795 [PMID:23241029] |
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]
