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ChEMBL ligand: CHEMBL897 (Benemid, Benuryl, HC 5006, NSC-18786, P-(dipropylsulfamoyl)benzoic acid, Probalan, Probampicin, Probecid, Probenate, Probenecid, Probenecidum) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]