example 15 [WO2015079413] [Ligand Id: 12667] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL509624
  • OATP2B1/Solute carrier organic anion transporter family member 2B1 in Human [ChEMBL: CHEMBL1743124] [GtoPdb: 1224] [UniProtKB: O94956]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
OATP2B1/Solute carrier organic anion transporter family member 2B1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1743124] [GtoPdb: 1224] [UniProtKB: O94956]
ChEMBL Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay B 4.21 pIC50 61659.5 nM IC50 RSC Med Chem (2023) 14: 890-898 [PMID:37252098]
ChEMBL Inhibition of human OATP2B1 expressed in Flp-In-CHO cells assessed as inhibition of OATP2B1 mediated DBF uptake using DBF as fluorescent substrate incubated for 2 mins by BCA assay B 4.21 pIC50 61500 nM IC50 RSC Med Chem (2023) 14: 890-898 [PMID:37252098]
SYNJ1/Synaptojanin-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523136] [GtoPdb: 1461] [UniProtKB: O43426]
ChEMBL Inhibition of C-Myc/DDK-tagged human recombinant SYNJ1 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay B 4.8 pIC50 <=15900 nM IC50 US-20170042857-A1. Synaptojanin-2 inhibitors for use in the treatment of cancer (2017)
ChEMBL Inhibition of C-Myc/DDK-tagged human recombinant SYNJ1 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay B 4.8 pIC50 <=15900 nM IC50 WO-2015079413-A2. Synaptojanin-2 inhibitors and uses thereof (2015)
SYNJ2/Synaptojanin-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523129] [GtoPdb: 1462] [UniProtKB: O15056]
ChEMBL Inhibition of C-Myc/DDK-tagged human recombinant SYNJ2 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay B 6.06 pIC50 874 nM IC50 US-20170042857-A1. Synaptojanin-2 inhibitors for use in the treatment of cancer (2017)
ChEMBL Inhibition of C-Myc/DDK-tagged human recombinant SYNJ2 expressed in HEK293T cells assessed as reduction in 5'-phosphatase activity incubated for 8 mins using fluorescently-labeled PI(3,4)P2 probe and Tapp1 PH-domain as detector protein by fluorescence polarization competitive assay B 6.06 pIC50 874 nM IC50 WO-2015079413-A2. Synaptojanin-2 inhibitors and uses thereof (2015)
ChEMBL Inhibition of recombinant full length C-Myc/DDK-tagged human SYNJ2 expressed in HEK293T cells using PI(3,4,5)P3 as substrate incubated for 8 mins assessed as hydrolysis of PI(3,4,5)P3 to PI(3,4)P2 by fluorescence polarization assay B 6.06 pIC50 874 nM IC50 US-20170165285-A1. Methods of preventing tumor metastasis, treating and prognosing cancer and identifying agents which are putative metastasis inhibitors (2017)
GtoPdb Inhibition of 5'-phosphatase activity in HEK293T cells expressing hSYNJ2 by fluorescence polarization competitive assay. - 6.06 pIC50 874 nM IC50 WO2015079413A2. Synaptojanin-2 inhibitors and uses thereof (2015)

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]