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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 |
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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 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]