probenecid [Ligand Id: 4357] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL897 (Benemid, Benuryl, HC 5006, NSC-18786, P-(dipropylsulfamoyl)benzoic acid, Probalan, Probampicin, Probecid, Probenate, Probenecid, Probenecidum)
  • ABCC2/Canalicular multispecific organic anion transporter 1 in Human [ChEMBL: CHEMBL5748] [GtoPdb: 780] [UniProtKB: Q92887]
  • ABCC2/Canalicular multispecific organic anion transporter 1 in Rat [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
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  • carbonic anhydrase 1/Carbonic anhydrase I in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
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  • carbonic anhydrase 9/Carbonic anhydrase IX in Human [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
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  • carbonic anhydrase 12/Carbonic anhydrase XII in Human [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
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  • Organic anion transporter 4/Solute carrier family 22 member 11 in Human [ChEMBL: CHEMBL2073677] [GtoPdb: 1030] [UniProtKB: Q9NSA0]
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  • Urate anion exchanger 1/Solute carrier family 22 member 12 in Human [ChEMBL: CHEMBL6120] [GtoPdb: 1031] [UniProtKB: Q96S37]
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  • OAT6/Solute carrier family 22 member 20 in Mouse [ChEMBL: CHEMBL5269] [GtoPdb: 1037] [UniProtKB: Q80UJ1]
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  • Organic anion transporter 1/Solute carrier family 22 member 6 in Human [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8]
  • Organic anion transporter 1/Solute carrier family 22 member 6 in Mouse [ChEMBL: CHEMBL5653] [GtoPdb: 1025] [UniProtKB: Q8VC69]
  • Organic anion transporter 1/Solute carrier family 22 member 6 in Rat [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956]
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  • Organic anion transporter 3/Solute carrier family 22 member 8 in Human [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7]
  • Organic anion transporter 3/Solute carrier family 22 member 8 in Rat [ChEMBL: CHEMBL2073666] [GtoPdb: 1027] [UniProtKB: Q9R1U7]
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  • Solute carrier organic anion transporter family member 1A1 in Rat [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
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  • Solute carrier organic anion transporter family member 1A4 in Rat [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
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  • TRPV2 in Rat [GtoPdb: 508] [UniProtKB: Q9WUD2]
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  • TAS2R16 in Human [GtoPdb: 669] [UniProtKB: Q9NYV7]
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  • TAS2R38 in Human [GtoPdb: 682] [UniProtKB: P59533]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ABCC2/Canalicular multispecific organic anion transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5748] [GtoPdb: 780] [UniProtKB: Q92887]
ChEMBL TP_TRANSPORTER: inhibition of SN-38 uptake in bile canalicular membrane vesicles F 4.37 pKi 42200 nM Ki Drug Metabol Pharmacokin (2002) 17: 23-33 [PMID:15618649]
ABCC2/Canalicular multispecific organic anion transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073676] [GtoPdb: 780] [UniProtKB: Q63120]
ChEMBL TP_TRANSPORTER: inhibition of DNP-SG uptake in blie canalicular membrane vesicle from SD rat F 4.35 pKi 44600 nM Ki Drug Metabol Pharmacokin (2002) 17: 23-33 [PMID:15618649]
carbonic anhydrase 1/Carbonic anhydrase I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
ChEMBL Inhibition of recombinant human carbonic anhydrase 1 after 15 mins by stopped flow CO2 hydration assay B 5 pKi >10000 nM Ki Bioorg Med Chem (2014) 22: 3982-3988 [PMID:25027802]
ChEMBL Inhibition of human carbonic anhydrase 1 by stopped-flow CO2 hydrase assay B 5 pKi >10000 nM Ki Bioorg Med Chem (2015) 23: 2975-2981 [PMID:26007302]
ChEMBL Inhibition of human carbonic anhydrase-1 incubated for 15 mins by stopped-flow CO2 hydration assay B 5 pKi >10000 nM Ki Bioorg Med Chem (2015) 23: 5311-5318 [PMID:26264840]
carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
ChEMBL Inhibition of recombinant human carbonic anhydrase 2 after 15 mins by stopped flow CO2 hydration assay B 6.37 pKi 431 nM Ki Bioorg Med Chem (2014) 22: 3982-3988 [PMID:25027802]
ChEMBL Inhibition of human carbonic anhydrase 2 by stopped-flow CO2 hydrase assay B 6.37 pKi 431 nM Ki Bioorg Med Chem (2015) 23: 2975-2981 [PMID:26007302]
ChEMBL Inhibition of human carbonic anhydrase-2 incubated for 15 mins by stopped-flow CO2 hydration assay B 6.37 pKi 431 nM Ki Bioorg Med Chem (2015) 23: 5311-5318 [PMID:26264840]
carbonic anhydrase 9/Carbonic anhydrase IX in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
ChEMBL Inhibition of recombinant human carbonic anhydrase 9 after 15 mins by stopped flow CO2 hydration assay B 6.44 pKi 360 nM Ki Bioorg Med Chem (2014) 22: 3982-3988 [PMID:25027802]
ChEMBL Inhibition of human carbonic anhydrase 9 by stopped-flow CO2 hydrase assay B 6.44 pKi 360 nM Ki Bioorg Med Chem (2015) 23: 2975-2981 [PMID:26007302]
ChEMBL Inhibition of human carbonic anhydrase-9 incubated for 15 mins by stopped-flow CO2 hydration assay B 6.44 pKi 360 nM Ki Bioorg Med Chem (2015) 23: 5311-5318 [PMID:26264840]
carbonic anhydrase 12/Carbonic anhydrase XII in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
ChEMBL Inhibition of recombinant human carbonic anhydrase 12 after 15 mins by stopped flow CO2 hydration assay B 5.9 pKi 1245 nM Ki Bioorg Med Chem (2014) 22: 3982-3988 [PMID:25027802]
ChEMBL Inhibition of human carbonic anhydrase 12 by stopped-flow CO2 hydrase assay B 5.9 pKi 1245 nM Ki Bioorg Med Chem (2015) 23: 2975-2981 [PMID:26007302]
ChEMBL Inhibition of human carbonic anhydrase-12 incubated for 15 mins by stopped-flow CO2 hydration assay B 5.9 pKi 1245 nM Ki Bioorg Med Chem (2015) 23: 5311-5318 [PMID:26264840]
Organic anion transporter 4/Solute carrier family 22 member 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073677] [GtoPdb: 1030] [UniProtKB: Q9NSA0]
ChEMBL TP_TRANSPORTER: inhibition of E1S uptake in OAT4-expressing S2 cells F 4.26 pKi 54900 nM Ki J Pharmacol Exp Ther (2002) 301: 797-802 [PMID:12023506]
ChEMBL TP_TRANSPORTER: inhibition of Ochratoxin A uptake in OAT4-expressing S2 cells F 4.35 pKi 44400 nM Ki Biochim Biophys Acta (2002) 1590: 64-75 [PMID:12063169]
ChEMBL Inhibition of OAT4 (unknown origin) B 4.26 pIC50 54900 nM IC50 Eur J Med Chem (2019) 166: 186-196 [PMID:30769179]
ChEMBL TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT4-expressing S2 cells F 4.6 pIC50 25400 nM IC50 J Pharmacol Sci (2004) 94: 197-202 [PMID:14978359]
Urate anion exchanger 1/Solute carrier family 22 member 12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6120] [GtoPdb: 1031] [UniProtKB: Q96S37]
ChEMBL Inhibition of human URAT1 expressed in xenopus oocyte assessed as inhibition of [14C]-labelled urate uptake after 60 mins by liquid scintillation counting B 4.06 pIC50 86390 nM IC50 J Med Chem (2011) 54: 2701-2713 [PMID:21449597]
ChEMBL Inhibition of human URAT1-mediated urate uptake in HEK293 cells B 4.3 pIC50 50000 nM IC50 Drug Metab Dispos (2007) 35: 981-986 [PMID:17325024]
ChEMBL Inhibition of URAT1 (unknown origin) B 4.82 pIC50 15000 nM IC50 Medchemcomm (2016) 7: 1587-1595
OAT6/Solute carrier family 22 member 20 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5269] [GtoPdb: 1037] [UniProtKB: Q80UJ1]
ChEMBL Inhibition of mouse Oat6-mediated [3H]ES uptake in Xenopus oocytes after 1 hr B 5.07 pKi 8511.38 nM Ki J Biol Chem (2007) 282: 23841-23853 [PMID:17553798]
ChEMBL Inhibition of mouse Oat6-mediated [3H]ES uptake in Xenopus oocytes after 1 hr B 5.08 pKi 8400 nM Ki J Biol Chem (2007) 282: 23841-23853 [PMID:17553798]
Organic anion transporter 1/Solute carrier family 22 member 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641347] [GtoPdb: 1025] [UniProtKB: Q4U2R8]
ChEMBL TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing S2 cells F 4.92 pKi 12100 nM Ki Eur J Pharmacol (2001) 419: 113-120 [PMID:11426832]
ChEMBL TP_TRANSPORTER: inhibition of Ochratoxin A uptake in OAT1-expressing S2 cells F 5.36 pKi 4410 nM Ki Life Sci (2001) 69: 2123-2135 [PMID:11669456]
ChEMBL TP_TRANSPORTER: inhibition of PAH uptake in OAT1-expressing CHO cells F 5.37 pKi 4300 nM Ki Anal Biochem (2000) 283: 49-55 [PMID:10929807]
GtoPdb - - 4.9 pIC50 12500 nM IC50 Kidney Int (2003) 63: 143-55 [PMID:12472777]
ChEMBL TP_TRANSPORTER: inhibition of Urate uptake (Urate: 300 uM) in OAT1-expressing S2 cells F 4.9 pIC50 12500 nM IC50 Kidney Int (2003) 63: 143-155 [PMID:12472777]
ChEMBL TP_TRANSPORTER: inhibition of PHA uptake (PHA: 5uM) in hOAT1-expressing S2 cells F 4.91 pIC50 12300 nM IC50 J Pharmacol Sci (2004) 94: 197-202 [PMID:14978359]
ChEMBL Inhibition of OAT1 (unknown origin) B 4.92 pIC50 12100 nM IC50 Eur J Med Chem (2019) 166: 186-196 [PMID:30769179]
ChEMBL TP_TRANSPORTER: inhibition of Adefovir uptake in OAT1-expressing CHO cells F 5.13 pIC50 7400 nM IC50 J Pharmacol Exp Ther (2000) 295: 10-15 [PMID:10991954]
ChEMBL TP_TRANSPORTER: inhibition of 6-Carboxyfluorescein uptake in OAT1-expressing CHO cells F 5.2 pIC50 6300 nM IC50 Anal Biochem (2000) 283: 49-55 [PMID:10929807]
Organic anion transporter 1/Solute carrier family 22 member 6 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5653] [GtoPdb: 1025] [UniProtKB: Q8VC69]
ChEMBL Inhibition of mouse Oat1-mediated [3H]PAH uptake in Xenopus oocytes after 1 hr B 5.19 pKi 6400 nM Ki J Biol Chem (2007) 282: 23841-23853 [PMID:17553798]
ChEMBL Inhibition of mouse Oat1-mediated [3H]PAH uptake in Xenopus oocytes after 1 hr B 5.2 pKi 6309.57 nM Ki J Biol Chem (2007) 282: 23841-23853 [PMID:17553798]
Organic anion transporter 1/Solute carrier family 22 member 6 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1777665] [GtoPdb: 1025] [UniProtKB: O35956]
ChEMBL TP_TRANSPORTER: inhibition of PAH uptake in Oat1-expressing LLC-PK1 cells F 4.51 pKi 31000 nM Ki J Pharmacol Exp Ther (2001) 298: 316-322 [PMID:11408557]
ChEMBL TP_TRANSPORTER: inhibition of PAH uptake in Xenopus laevis oocytes F 4.8 pKi 15800 nM Ki Eur J Pharmacol (2000) 409: 31-36 [PMID:11099697]
Organic anion transporter 3/Solute carrier family 22 member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1641348] [GtoPdb: 1027] [UniProtKB: Q8TCC7]
ChEMBL TP_TRANSPORTER: inhibition of MTX uptake in OAT3-expressing S2 cells F 4.53 pKi 29800 nM Ki J Pharmacol Exp Ther (2002) 302: 666-671 [PMID:12130730]
ChEMBL TP_TRANSPORTER: inhibition of E1S uptake in OAT3-expressing S2 cells F 5.05 pKi 9000 nM Ki Eur J Pharmacol (2001) 419: 113-120 [PMID:11426832]
ChEMBL TP_TRANSPORTER: inhibition of Ochratoxin A uptake in OAT3-expressing S2 cells F 5.36 pKi 4410 nM Ki Life Sci (2001) 69: 2123-2135 [PMID:11669456]
ChEMBL Inhibition of OAT3 (unknown origin) B 5.05 pIC50 9000 nM IC50 Eur J Med Chem (2019) 166: 186-196 [PMID:30769179]
ChEMBL TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in hOAT3-expressing S2 cells F 5.31 pIC50 4930 nM IC50 J Pharmacol Sci (2004) 94: 197-202 [PMID:14978359]
Organic anion transporter 3/Solute carrier family 22 member 8 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073666] [GtoPdb: 1027] [UniProtKB: Q9R1U7]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake in Oat3-expressing LLC-PK1 cells F 4.7 pKi 20000 nM Ki J Pharmacol Exp Ther (2001) 298: 316-322 [PMID:11408557]
ChEMBL TP_TRANSPORTER: inhibition of PCG uptake in Oat3-expressing LLC-PK1 cells F 5.35 pKi 4430 nM Ki Mol Pharmacol (2002) 61: 982-988 [PMID:11961115]
ChEMBL TP_TRANSPORTER: inhibition of ES uptake (ES: 50nM) in rOAT3-expressing S2 cells F 5.22 pIC50 6030 nM IC50 J Pharmacol Sci (2004) 94: 197-202 [PMID:14978359]
Solute carrier organic anion transporter family member 1A1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp1-expressing LLC-PK1 cells F 4.13 pKi 74400 nM Ki J Pharmacol Exp Ther (2001) 298: 316-322 [PMID:11408557]
Solute carrier organic anion transporter family member 1A4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
ChEMBL TP_TRANSPORTER: inhibition of E217betaG uptake in Oatp2-expressing LLC-PK1 cells F 4.14 pKi 72900 nM Ki J Pharmacol Exp Ther (2001) 298: 316-322 [PMID:11408557]
UDP-glucuronosyltransferase 1-7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743317] [UniProtKB: Q9HAW7]
ChEMBL Inhibition of 4-methylumbelliferone glucuronidation by human recombinant UGT1A7 B 4.02 pKi 96000 nM Ki Pharmacol Ther (2005) 106: 97-132 [PMID:15781124]
TRPV2 in Rat [GtoPdb: 508] [UniProtKB: Q9WUD2]
GtoPdb - - 4.5 pEC50 31900 nM EC50 Neurosci Lett (2007) 425: 120-5 [PMID:17850966]
TAS2R16 in Human [GtoPdb: 669] [UniProtKB: Q9NYV7]
GtoPdb - - 3.53 pIC50 292000 nM IC50 PLoS One (2011) 6: e20123 [PMID:21629661]
TAS2R38 in Human [GtoPdb: 682] [UniProtKB: P59533]
GtoPdb - - 3.68 pIC50 211000 nM IC50 PLoS One (2011) 6: e20123 [PMID:21629661]

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]