BDBM50416875 AMG-073::AMG073 HCL::CINACALCET::CINACALCET HYDROCHLORIDE::US9487494, Cinacalcet

SMILES C[C@H](c1cccc2c1cccc2)NCCCc3cccc(c3)C(F)(F)F

InChI Key InChIKey=VDHAWDNDOKGFTD-UHFFFAOYSA-N

Data  3 IC50  4 EC50

PDB links: 6 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 7 hits for monomerid = 50416875   

TargetCytochrome P450 2D6(Human)
Leo Pharma

US Patent
LigandPNGBDBM50416875(CINACALCET | AMG-073 | AMG073 HCL | CINACALCET HYD...)
Affinity DataIC50: 50nMpH: 7.4 T: 2°CAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/2/2017
Entry Details
Go to US Patent

TargetGlycine receptor subunit alpha-1(Human)
University of Pittsburgh

Curated by ChEMBL
LigandPNGBDBM50416875(CINACALCET | AMG-073 | AMG073 HCL | CINACALCET HYD...)
Affinity DataEC50:  320nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/1/2016
Entry Details Article
PubMed
TargetExtracellular calcium-sensing receptor(Human)
Galapagos

Curated by ChEMBL
LigandPNGBDBM50416875(CINACALCET | AMG-073 | AMG073 HCL | CINACALCET HYD...)
Affinity DataEC50:  80nMAssay Description:Positive allosteric modulation of human CaSR transfected in CHO cells after 5 hrs by luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/24/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetExtracellular calcium-sensing receptor(Human)
Galapagos

Curated by ChEMBL
LigandPNGBDBM50416875(CINACALCET | AMG-073 | AMG073 HCL | CINACALCET HYD...)
Affinity DataEC50:  19.9nMAssay Description:Positive allosteric modulation of calcium sensing receptor by cell based assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetCytochrome P450 2D6(Human)
Leo Pharma

US Patent
LigandPNGBDBM50416875(CINACALCET | AMG-073 | AMG073 HCL | CINACALCET HYD...)
Affinity DataIC50: 100nMAssay Description:Inhibition of recombinant human CYP2D6 expressed in bacterial membranes using AMMC as substrate preincubated for 10 mins followed by NADPH addition m...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/3/2020
Entry Details Article
PubMed
TargetExtracellular calcium-sensing receptor(Human)
Galapagos

Curated by ChEMBL
LigandPNGBDBM50416875(CINACALCET | AMG-073 | AMG073 HCL | CINACALCET HYD...)
Affinity DataEC50:  180nMAssay 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...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/3/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetAngiotensin-converting enzyme 2(Human)
University of California San Francisco (Ucsf)

Curated by ChEMBL
LigandPNGBDBM50416875(CINACALCET | AMG-073 | AMG073 HCL | CINACALCET HYD...)
Affinity DataIC50: 2.82E+4nMAssay Description:Inhibition of recombinant human ACE2 using MCA-Tyr-Val-Ala-Asp-Ala-Pro-Lys(DNP)-OH as substrate preincubated for 15 mins followed by substrate additi...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/4/2023
Entry Details Article
PubMed