saridegib [Ligand Id: 8198] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL538867 (FIN-5, IP-9, IP9 FREE BASE, Ipi-926, IPI 926, IPI-926, IPI-926 FREE BASE, Patidegib, Saridegib)
  • Alkaline phosphatase, germ cell type in Human [ChEMBL: CHEMBL3402] [UniProtKB: P10696]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Alkaline phosphatase, germ cell type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3402] [UniProtKB: P10696]
ChEMBL Alkaline Phosphatase Assay: C3H10T1/2 cells were plated in 96 wells with a density of 8×103 cells/well. Cells were grown to confluence (72 hrs). After sonic Hedgehog (250 ng/ml), and/or compound treatment, the cells were lysed in 110 μL of lysis buffer (50 mm Tris ph 7.4, 0.1% tritonx100), plates were sonicated and lysates spun through 0.2 μm PVDF plates (Corning). 40 μL of lysates was assayed for AP activity in alkaline buffer solution (Sigma) containing 1 mg/ml p-Nitrophenyl Phosphate. After incubating for 30 min at 37° C., the plates were read on an Envision plate reader at 405 nm. Total protein was quantified with a BCA protein assay kit from Pierce according to manufacturer's instructions. B 7.7 pEC50 <20 nM EC50 US-10314827-B2. Methods of use of cyclopamine analogs (2019)
SMO/Protein smoothened in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5971] [GtoPdb: 239] [UniProtKB: Q99835]
GtoPdb - - 8.85 pIC50 1.4 nM IC50 J Med Chem (2009) 52: 4400-18 [PMID:19522463]
ChEMBL Inhibition of human recombinant SMO expressed in mouse C3H10T1/2 cells assessed as inhibition of association of BODIPY-cyclopamine B 8.85 pIC50 1.4 nM IC50 J Med Chem (2009) 52: 4400-4418 [PMID:19522463]

ChEMBL data shown on this page come from version 36:

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]