General Information of the Compound
Compound ID
CP0156217
Compound Name
APO-866
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Synonyms
APO-866
Daporinad
FK-866
WK-175
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Structure
Formula
C24H29N3O2
Molecular Weight
391.515
Canonical SMILES
O=C(NCCCCC1CCN(CC1)C(=O)c1ccccc1)\C=C\c1cccnc1
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InChI
InChI=1S/C24H29N3O2/c28-23(12-11-21-8-6-15-25-19-21)26-16-5-4-7-20-13-17-27(18-14-20)24(29)22-9-2-1-3-10-22/h1-3,6,8-12,15,19-20H,4-5,7,13-14,16-18H2,(H,26,28)/b12-11+
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InChIKey
KPBNHDGDUADAGP-VAWYXSNFSA-N
CAS
658084-64-1
Physicochemical Property
logP
3.9337
Rotatable Bonds
8
Heavy Atom Count
29
Polar Areas
62.3
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
3
Complexity
29

"RO5" indicates the cutoff set by lipinski's rule of five:

(1) Molecular weight less than 500 Dalton;

(2) xlogp less than 5;

(3) No more than 5 hbonddonor (Hydrogen Bond Donor Count);

(4) No more than 10 hbondacc (Hydrogen Bond Acceptor Count);

(5) No more than 10 rotbonds (Rotatable Bond Count).

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PubChem ID
CID: 6914657
SID: 14780790
ChEMBL ID
CHEMBL566757
DrugBank ID
DB12731
Map of Molecular Bioactivity Related to the Compound
Map of Molecular Bioactivity Related to the Compound

Compound
Cell Line
Protein

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Compound
Protein ID: PT01903, Nicotinamide phosphoribosyltransferase
Cell-based Assay
Cell Line ID Cell Line Name Cell Line Organism
CL000072 A2780 Homo sapiens (Human)  1
1
IC50 = 1 nM
   TI
   LI
   LO
   TS
CL000063 Hep-G2 Homo sapiens (Human)  1
1
IC50 = 2.2 nM
   TI
   LI
   LO
   TS
CL000154 HEK293-EBNA1-6E Homo sapiens (Human)  1
1
IC50 = 5 nM
   TI
   LI
   LO
   TS
Biochemical Assays
1 IC50 = 3 nM
2 IC50 = 6.8 nM
3 IC50 = 9 nM
4 IC50 = 20.7 nM
5 IC50 = 32 nM
6 IC50 = 35 nM
7 IC50 = 14800 nM
8 Ki = 0.3 nM
9 Ki = 3 nM
Cell Viability or Cytotoxicity Assay
Cell Line ID Cell Line Name Cell Line Organism
CL000004 SH-SY5Y Homo sapiens (Human)  1
1
EC50 = 3.2 nM
   TI
   LI
   LO
   TS
CL000072 A2780 Homo sapiens (Human)  1
1
IC50 = 1.6 nM
   TI
   LI
   LO
   TS
Clinical Information about the Compound
Drug 1 ( Daporinad )
Drug Name Daporinad
Company Astellas Pharma GmbH
Indication
leukaemia
Phase 2
Target(s)
Nicotinamide phosphoribosyltransferase (NAMPT)
Inhibitor