famotidine [Ligand Id: 7074] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL902 (Amfamox, Fadul, Famodil, Famosan, Famotidina, Famotidine, Famotidine component of duexis, Famotidine component of pepcid complete, Famotidine preservative free, Famotidine preservative free (pharmacy bulk), Famoxal, Fluxid, Ganor, Gaster, Gastridin, Gastropen, L 643341, Lecedil, MK-208, Motiax, Muclox, NSC-757810, Pepcid, Pepcid ac, Pepcidac, Pepcid ac (geltab), Pepcidine, Pepcid preservative free, Pepcid rpd, Pepdine, Pepdul, YM-11170)
  • carbonic anhydrase 1/Carbonic anhydrase 1 in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
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  • carbonic anhydrase 12/Carbonic anhydrase 12 in Human [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
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  • carbonic anhydrase 13/Carbonic anhydrase 13 in Human [ChEMBL: CHEMBL3912] [GtoPdb: 2748] [UniProtKB: Q8N1Q1]
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  • carbonic anhydrase 14/Carbonic anhydrase 14 in Human [ChEMBL: CHEMBL3510] [GtoPdb: 2598] [UniProtKB: Q9ULX7]
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  • carbonic anhydrase 2/Carbonic anhydrase 2 in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • carbonic anhydrase 4/Carbonic anhydrase 4 in Human [ChEMBL: CHEMBL3729] [GtoPdb: 2599] [UniProtKB: P22748]
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  • carbonic anhydrase 5A/Carbonic anhydrase 5A, mitochondrial in Human [ChEMBL: CHEMBL4789] [GtoPdb: 3093] [UniProtKB: P35218]
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  • Carbonic anhydrase 5B, mitochondrial in Human [ChEMBL: CHEMBL3969] [UniProtKB: Q9Y2D0]
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  • carbonic anhydrase 7/Carbonic anhydrase 7 in Human [ChEMBL: CHEMBL2326] [GtoPdb: 2749] [UniProtKB: P43166]
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  • carbonic anhydrase 9/Carbonic anhydrase 9 in Human [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
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  • H2 receptor/Histamine H2 receptor in Human [ChEMBL: CHEMBL1941] [GtoPdb: 263] [UniProtKB: P25021]
  • Histamine H2 receptor in Guinea pig [ChEMBL: CHEMBL2882] [UniProtKB: P47747]
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  • Multidrug and toxin extrusion/Multidrug and toxin extrusion protein 1 in Human [ChEMBL: CHEMBL1743126] [GtoPdb: 1216] [UniProtKB: Q96FL8]
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  • MATE2/Multidrug and toxin extrusion protein 2 in Human [ChEMBL: CHEMBL1743127] [GtoPdb: 1217] [UniProtKB: Q86VL8]
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  • POU domain, class 5, transcription factor 1 in Human [ChEMBL: CHEMBL3580526] [UniProtKB: Q01860]
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  • Organic cation transporter 2/Solute carrier family 22 member 2 in Human [ChEMBL: CHEMBL1743122] [GtoPdb: 1020] [UniProtKB: O15244]
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  • Organic cation transporter 3/Solute carrier family 22 member 3 in Human [ChEMBL: CHEMBL2073673] [GtoPdb: 1021] [UniProtKB: O75751]
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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 1 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 12/Carbonic anhydrase 12 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 13 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 14 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]
carbonic anhydrase 2/Carbonic anhydrase 2 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 3 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 4 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 5A/Carbonic anhydrase 5A, mitochondrial 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 5B, mitochondrial 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 6 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 7 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 9/Carbonic anhydrase 9 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]
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]
POU domain, class 5, transcription factor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3580526] [UniProtKB: Q01860]
ChEMBL OCT3 inhibitory activity: An existing amount of the OCT3 protein can be estimated from an amount of a compound free in the extracellular fluid in a method similar to a method described in Japanese Patent No. 1936624. In the experiment, HEK293 cells, which are human embryonic kidney cell lines expressing the human organic cation transporter 3 (OCT3) are prepared as a positive control, and cell lines the OCT3 expression of which is desired to be checked are prepared as test cells. The cells are seeded at 1.5×105 cells/well in a 24-well plate and cultured overnight in a carbon dioxide incubator. After being dissolved in a 100% DMSO solution, the test substance was dissolved in a HBSS-HEPES solution (a buffer solution adjusted to pH 7.4 with 1M sodium hydroxide, by dissolving 9.7 g of Hanks balanced salt, 25 mL of 1.4% sodium bicarbonate, and 25 mL of 1M HEPES in 940 mL of ultrapure water). After a cell culture medium is removed, a pretreatment for 5 minutes is performed with 1 mL of the HBSS-HEPES solution. Thereafter, the compound of the present invention as the test substance and histamine (final concentration: 100 nM) are added to the cells and allowed to react for 1 minute at room temperature. After completion of the reaction, the reaction is stopped with the ice-cooled HBSS-HEPES solution, and extracellular fluid is collected. B 4.17 pIC50 67600 nM IC50 US-10149840-B2. OCT3 activity inhibitor containing imidazopyridine derivative as active component, and OCT3 detection agent (2018)
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 36:

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]