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AZD3965 | AZD3965 : Inhibitor of SLC16A1
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
SLC16A1
  • Ki:1.6 nM
  • Ki:3.2 nM
  • IC50:5.12 nM
  • GI50:12.35 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
SLC16A7

Gene ID: O60669

Organism: Homo sapiens

Family: Monocarboxylate porter (TC 2.A.1.13) family

Potency: Ki - 20 nM

Selectivity Assessment Description:
No inhibition of lactate transport mediated by MCT3 or MCT4 w in the MCT1, MCT2, MCT3 and MCT4 null ...

Potency
Cellular
In Vitro

SLC16A1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.18632/oncotarget.18215

In Vivo Validations

Mouse
Dose: 10 mg/Kg
Route of delivery: Intravenous
Plasma half life: 2.91 h
Systemic clearance: 56.1 ml/h
Cmax: 4.02 ug/ml
Area Under the Curve:: 4.94 ug*h/ml
Volume of Distribution at Steady-State: 44.2 ml/Kg

DOI Reference: 10.1007/s11095-019-2735-z

Dose: 100 mg/Kg
Route of delivery: Oral
Plasma half life: 4.46 h
Systemic clearance: 26.6 ml/h
Cmax: 30.3 ug/ml
Area Under the Curve:: 71.4 ug*h/ml

DOI Reference: 10.1007/s11095-019-2735-z

Chemical Information

Molecular Formula C21H24F3N5O5S
SMILEs Cc1[nH]nc(C(F)(F)F)c1Cc1sc2c(c1C(=O)N1C[C@](C)(O)CO1)c(=O)n(C)c(=O)n2C(C)C
InChI InChI=1S/C21H24F3N5O5S/c1-9(2)29-18-14(16(30)27(5)19(29)32)13(17(31)28-7-20(4,33)8-34-28)12(35-18)6-11-10(3)25-26-15(11)21(22,23)24/h9,33H,6-8H2,1-5H3,(H,25,26)/t20-/m0/s1
Molecular weight 515.15 Da
AlogP 0.0
HBond acceptors 10
HBond donors 2
Atoms 59

Vendors

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Expert Reviews

by SERP
(on 6 Feb 2023 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
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