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

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ChEMBL ligand: CHEMBL897 (Probalan, HC 5006, NSC-18786, Benemid, Probenecid, Probampicin, Benuryl, Probecid)
  • 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]
  • 4.35
1 CHEMBL897_lig_chart_1 Canalicular multispecific organic anion transporter 1 HumanRat
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  • carbonic anhydrase 1/Carbonic anhydrase I in Human [ChEMBL: CHEMBL261] [GtoPdb: 2597] [UniProtKB: P00915]
  • 5
2 CHEMBL897_lig_chart_2 Carbonic anhydrase I Human
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  • carbonic anhydrase 2/Carbonic anhydrase II in Human [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918]
  • 6.37
3 CHEMBL897_lig_chart_3 Carbonic anhydrase II Human
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  • carbonic anhydrase 9/Carbonic anhydrase IX in Human [ChEMBL: CHEMBL3594] [GtoPdb: 3055] [UniProtKB: Q16790]
  • 6.44
4 CHEMBL897_lig_chart_4 Carbonic anhydrase IX Human
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  • carbonic anhydrase 12/Carbonic anhydrase XII in Human [ChEMBL: CHEMBL3242] [GtoPdb: 2747] [UniProtKB: O43570]
  • 5.9
5 CHEMBL897_lig_chart_5 Carbonic anhydrase XII Human
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  • Organic anion transporter 4/Solute carrier family 22 member 11 in Human [ChEMBL: CHEMBL2073677] [GtoPdb: 1030] [UniProtKB: Q9NSA0]
  • 4.31
6 CHEMBL897_lig_chart_6 Solute carrier family 22 member 11 Human
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  • Urate anion exchanger 1/Solute carrier family 22 member 12 in Human [ChEMBL: CHEMBL6120] [GtoPdb: 1031] [UniProtKB: Q96S37]
  • This target only has 0 pki data point
  • 0
7 CHEMBL897_lig_chart_7 Solute carrier family 22 member 12 Human
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  • OAT6/Solute carrier family 22 member 20 in Mouse [ChEMBL: CHEMBL5269] [GtoPdb: 1037] [UniProtKB: Q80UJ1]
  • 5.07
8 CHEMBL897_lig_chart_8 Solute carrier family 22 member 20 Mouse
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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]
  • 4.65
9 CHEMBL897_lig_chart_9 Solute carrier family 22 member 6 HumanMouseRat
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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]
  • 5.03
10 CHEMBL897_lig_chart_10 Solute carrier family 22 member 8 HumanRat
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  • Solute carrier organic anion transporter family member 1A1 in Rat [ChEMBL: CHEMBL1781859] [UniProtKB: P46720]
  • This target only has 1 pki data point
  • 4.13
11 CHEMBL897_lig_chart_11 Solute carrier organic anion transporter family member 1A1 Rat
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  • Solute carrier organic anion transporter family member 1A4 in Rat [ChEMBL: CHEMBL1781860] [UniProtKB: O35913]
  • This target only has 1 pki data point
  • 4.14
12 CHEMBL897_lig_chart_12 Solute carrier organic anion transporter family member 1A4 Rat
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  • UDP-glucuronosyltransferase 1-7 in Human [ChEMBL: CHEMBL1743317] [UniProtKB: Q9HAW7]
  • This target only has 1 pki data point
  • 4.02
13 CHEMBL897_lig_chart_13 UDP-glucuronosyltransferase 1-7 Human
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  • TRPV2 in Rat [GtoPdb: 508] [UniProtKB: Q9WUD2]
  • This target only has 0 pki data point
  • 0
14 CHEMBL897_lig_chart_14 TRPV2 Rat
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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 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 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 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 Pharmacology and Therapeutics (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]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]