BDBM50416875 AMG-073::AMG073 HCL::CINACALCET::CINACALCET HYDROCHLORIDE::US9487494, Cinacalcet
SMILES: C[C@@H](NCCCc1cccc(c1)C(F)(F)F)c1cccc2ccccc12
InChI Key: InChIKey=VDHAWDNDOKGFTD-MRXNPFEDSA-N
Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kcal/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Cytochrome P450 2D6 (Homo sapiens (Human)) | BDBM50416875 (AMG-073 | AMG073 HCL | CINACALCET | CINACALCET HYD...) | PDB UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase DrugBank PC cid PC sid PDB UniChem Similars | US Patent | n/a | n/a | 50 | n/a | n/a | n/a | n/a | 7.4 | 37 |
LEO PHARMA A/S US Patent | Assay Description Incubations were conducted in 96 well microtiter plates based on a method described by BD Biosciences. To the first well in each row, a NADPH regener... | US Patent US9487494 (2016) BindingDB Entry DOI: 10.7270/Q21V5CX3 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Glycine receptor subunit alpha-1 (Homo sapiens (Human)) | BDBM50416875 (AMG-073 | AMG073 HCL | CINACALCET | CINACALCET HYD...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase DrugBank PC cid PC sid PDB UniChem Similars | Article PubMed | n/a | n/a | n/a | n/a | 320 | n/a | n/a | n/a | n/a |
University of Pittsburgh Curated by ChEMBL | Assay Description Potentiation of human GlyR-alpha1 expressed in Xenopus laevis oocytes assessed as induction of glycine-activated currents after 1 to 4 days by two-el... | J Med Chem 58: 2958-66 (2015) Article DOI: 10.1021/jm501873p BindingDB Entry DOI: 10.7270/Q22F7Q4V | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Calcium-sensing receptor (CaSR) (Homo sapiens (Human)) | BDBM50416875 (AMG-073 | AMG073 HCL | CINACALCET | CINACALCET HYD...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase DrugBank PC cid PC sid PDB UniChem Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 180 | n/a | n/a | n/a | n/a |
Mitsubishi Tanabe Pharma Corporation Curated by ChEMBL | Assay Description Agonist activity at human CaSR expressed in CHO cells assessed as increase in intracellular calcium mobilization after 1 hr by Fura-2 dye-based fluor... | Bioorg Med Chem Lett 28: 2055-2060 (2018) Article DOI: 10.1016/j.bmcl.2018.04.055 BindingDB Entry DOI: 10.7270/Q2DF6TP0 | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Calcium-sensing receptor (CaSR) (Homo sapiens (Human)) | BDBM50416875 (AMG-073 | AMG073 HCL | CINACALCET | CINACALCET HYD...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase DrugBank PC cid PC sid PDB UniChem Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 19.9 | n/a | n/a | n/a | n/a |
ACADIA Pharmaceuticals AB Curated by ChEMBL | Assay Description Positive allosteric modulation of calcium sensing receptor by cell based assay | Bioorg Med Chem Lett 20: 5918-21 (2010) Article DOI: 10.1016/j.bmcl.2010.07.077 BindingDB Entry DOI: 10.7270/Q22J6D4S | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) | ||||||||||||
Cytochrome P450 2D6 (Homo sapiens (Human)) | BDBM50416875 (AMG-073 | AMG073 HCL | CINACALCET | CINACALCET HYD...) | PDB UniProtKB/SwissProt UniProtKB/TrEMBL GoogleScholar AffyNet | Purchase DrugBank PC cid PC sid PDB UniChem Similars | Article PubMed | n/a | n/a | <100 | n/a | n/a | n/a | n/a | n/a | n/a |
Mitsubishi Tanabe Pharma Corporation Curated by ChEMBL | Assay Description Inhibition of recombinant human CYP2D6 expressed in bacterial membranes using AMMC as substrate preincubated for 10 mins followed by NADPH addition m... | Bioorg Med Chem Lett 28: 2055-2060 (2018) Article DOI: 10.1016/j.bmcl.2018.04.055 BindingDB Entry DOI: 10.7270/Q2DF6TP0 | |||||||||||
More data for this Ligand-Target Pair | |||||||||||||
Calcium-sensing receptor (CaSR) (Homo sapiens (Human)) | BDBM50416875 (AMG-073 | AMG073 HCL | CINACALCET | CINACALCET HYD...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase DrugBank PC cid PC sid PDB UniChem Similars | PDB Article PubMed | n/a | n/a | n/a | n/a | 80 | n/a | n/a | n/a | n/a |
Galapagos SASU Curated by ChEMBL | Assay Description Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assay | Bioorg Med Chem Lett 23: 2451-4 (2013) Article DOI: 10.1016/j.bmcl.2013.01.078 BindingDB Entry DOI: 10.7270/Q2930VJZ | |||||||||||
More data for this Ligand-Target Pair | 3D Structure (crystal) |