tacrine
A cholinesterase inhibitor that crosses the blood-brain barrier. Tacrine has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders.
Ligand Summary
UNII: 4VX7YNB537
PubChem: 135504745
PubChem: 1935
PubChem: 6420002
Guide to Pharmacology: 6687
ChEMBL: CHEMBL1677
ChEMBL: CHEMBL95
ChEMBL: CHEMBL1337960
DrugCentral: 2551
LyCHI: 5L7ZPW8RPXA9
Target Activities
ACHE
Acetylcholinesterase
166 Activities
Items per page:
1 – 10 of 166
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.5 | |||||
IC50 | 8.5 | Eur. J. Med. Chem., (2011) 46:8:3250 | ||||
IC50 | 8.12 | Bioorg. Med. Chem., (2016) 24:10:2318 | ||||
Ki | 8.12 | Bioorg. Med. Chem., (2016) 24:10:2318 | ||||
IC50 | 7.9 | J Med Chem, (2019) 62:20:9078 | ||||
IC50 | 7.73 | J Med Chem, (2018) 61:4:1646 | ||||
IC50 | 7.7 | J Med Chem, (2018) 61:4:1646 | ||||
IC50 | 7.52 | Bioorg. Med. Chem. Lett., (1996) 6:6:737 | ||||
IC50 | 7.52 | Bioorg Med Chem, (2019) 27:6:895 | ||||
Ki | 7.49 | Bioorg. Med. Chem., (2012) 20:22:6739 | ||||
BCHE
Cholinesterase
109 Activities
Items per page:
1 – 10 of 109
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 7.2 | |||||
IC50 | 10.57 | Eur. J. Med. Chem., (2011) 46:8:3250 | ||||
IC50 | 9.05 | Bioorg. Med. Chem. Lett., (2003) 13:14:2389 | ||||
IC50 | 8.29 | J. Med. Chem., (2008) 51:4:713 | ||||
IC50 | 8.22 | J. Med. Chem., (1995) 38:7:1084 | ||||
IC50 | 8.22 | J. Med. Chem., (1995) 38:15:2802 | ||||
Ki | 8.15 | J. Med. Chem., (2006) 49:11:3421 | ||||
Ki | 8.15 | Bioorg. Med. Chem. Lett., (2008) 18:19:5213 | ||||
Ki | 8.15 | J. Med. Chem., (2008) 51:11:3154 | ||||
Ki | 8.06 | Bioorg. Med. Chem., (2012) 20:22:6739 | ||||
CHRNE
Acetylcholine receptor subunit epsilon
2 Activities
APP
Amyloid-beta A4 protein
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.91 | Eur. J. Med. Chem., (2016) 116:None:200 | ||||
IC50 | 7.91 | |||||
SLC6A2
Sodium-dependent noradrenaline transporter
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.29 | None, None:None:None | ||||
Ki | 6.29 | None, None:None:None | ||||
CYP1A2
Cytochrome P450 1A2
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
AC50 | 6.3 | None, None:None:None | ||||
AC50 | 6.1 | None, None:None:None | ||||
CHRM1
Muscarinic acetylcholine receptor M1
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.7 | |||||
CHRM2
Muscarinic acetylcholine receptor M2
1 Activities
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1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 5.68 | |||||
SLC22A2
Solute carrier family 22 member 2
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.17 | J. Med. Chem., (2011) 54:13:4548 | ||||
CYP2D6
Cytochrome P450 2D6
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.52 | None, None:None:None | ||||