Compound Detail

CHEMBL1201092

RIVASTIGMINE TARTRATE

💊 Approved Drug

Enter ChEMBL ID:

Free Research Context This compound will appear in recent viewed items on the research home for this browser.

Research home View demo workspace

💊 Approved Drug

CCN(C)C(=O)Oc1cccc([C@H](C)N(C)C)c1.O=C(O)[C@H](O)[C@@H](O)C(=O)O

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL1201092
Name	RIVASTIGMINE TARTRATE
Phase	Approved
Structure Type	MOL
InChI Key	GWHQHAUAXRMMOT-MBANBULQSA-N
Therapeutic	✓ Yes
Parent Compound	CHEMBL636
Active Moiety	CHEMBL636

Known Names

ENA 713 Exelon Exelon tartrate Nimvastid Prometax Rivastigmine 1 a pharma Rivastigmine actavis Rivastigmine bitartrate Rivastigmine hexal Rivastigmine hydrogen tartrate Rivastigmine hydrogentartrate Rivastigmine sandoz +3 more

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Mechanisms

Molecular Properties

250.3

MW (Da)

2.76

ALogP

HBA

HBD

32.8

PSA (Å²)

0.82

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
First Approval	1998
Availability	Prescription
Chirality	Single Enantiomer

Routes of Administration

Oral

USAN Stem

-stigmine

Extended Properties

Molecular Formula	C18H28N2O8
MW	400.43
Aromatic Rings	1
Heavy Atoms	18
NP-Likeness	-0.98

Mechanism of Action

Mechanism	Action Type	Target	Direct	Efficacy
Cholinesterases; ACHE & BCHE inhibitor	INHIBITOR	Cholinesterases; ACHE & BCHE	✓	✓

Indications

Alzheimer Disease Dementia Parkinson Disease Hypotension, Orthostatic

Activity Summary

IC50 7 meas. best 6.3

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Cholinesterase CHEMBL5763	IC50	6.3	6.3	499.0	1
Cholinesterase CHEMBL1914	IC50	5.84	5.84	1439.0	1
Acetylcholinesterase CHEMBL220	IC50	5.19	4.945	6500.0	2
MAP/microtubule affinity-regulating kinase 4 CHEMBL5754	IC50	5.17	5.17	6740.0	1
Acetylcholinesterase CHEMBL4078	IC50	4.21	4.21	62400.0	1

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Cholinesterase	IC50	=	499.0	nM	6.3	Inhibition of equine serum butyrylcholine esterase incubated for 15 mins using S...	25768702
Cholinesterase	IC50	=	1439.0	nM	5.84	Inhibition of human BuchE using butyrylthiocholine iodide as substrate preincuba...	32380361
Acetylcholinesterase	IC50	=	6500.0	nM	5.19	Inhibition of human AChE using acetylthiocholine iodide as substrate preincubate...	27951490
MAP/microtubule affinity-regulating kinase 4	IC50	=	6740.0	nM	5.17	Inhibition of human MARK4 expressed in Escherichia coli preincubated for 1 hr fo...	38911173
Acetylcholinesterase	IC50	=	19800.0	nM	4.7	Inhibition of human AChE using acetylthiocholine iodide as substrate preincubate...	32380361
Acetylcholinesterase	IC50	=	62400.0	nM	4.21	Inhibition of electric eel AChE incubated for 15 mins using acetylcholine iodide...	25768702

Literature References

PubMed	DOI	Target Context	# Activities
16913695	10.1021/jm060293s	Acetylcholinesterase	2
25768702	10.1016/j.ejmech.2015.02.055	Acetylcholinesterase	1
25768702	10.1016/j.ejmech.2015.02.055	Cholinesterase	1
25768702	10.1016/j.ejmech.2015.02.055	Unchecked	1
27951490	10.1016/j.ejmech.2016.12.005	Acetylcholinesterase	1
27951490	10.1016/j.ejmech.2016.12.005	Cholinesterase	1
32380361	10.1016/j.ejmech.2020.112282	Amine oxidase [flavin-containing] B	1
32380361	10.1016/j.ejmech.2020.112282	Acetylcholinesterase	1
32380361	10.1016/j.ejmech.2020.112282	Cholinesterase	1
32380361	10.1016/j.ejmech.2020.112282	Unchecked	1
38911173	10.1039/d4md00059e	MAP/microtubule affinity-regulating kinase 4	1

Data from ChEMBL 36 via Core Engine