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Compound Detail

CHEMBL64894

GENTIAN VIOLET
💊 Approved Drug
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💊 Approved Drug
CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1.[Cl-]

Basic Information

ChEMBL ID CHEMBL64894
Name GENTIAN VIOLET
Phase Approved
Structure Type MOL
InChI Key ZXJXZNDDNMQXFV-UHFFFAOYSA-M
Therapeutic ✓ Yes
Parent Compound CHEMBL459265
Active Moiety CHEMBL459265

Known Names

Basic violet 1 Basic violet 3 C.i. 42535 C.i. basic violet 1 C.i. basic violet 3 Chlorure de methylrosanilinium Ci 42535 Cloruro de metilrosanilina Crystal violet Genapax Gentian violet GNF-Pf-880 +11 more
39
Targets
89
Activities
4
Assay Types
0
PK Parameters
20
Publications
23
Known Names
3
Indications
1
Mechanisms

Molecular Properties

372.5
MW (Da)
4.46
ALogP
2
HBA
0
HBD
9.5
PSA (Ų)
0.73
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1982
Availability Withdrawn
Chirality Achiral

Routes of Administration

Topical

Flags

Withdrawn Natural Product

Extended Properties

Molecular Formula C25H30ClN3
MW 407.99
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.31

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
DNA inhibitor INHIBITOR DNA

Indications

Candidiasis, Oral HIV Infections Hidradenitis Suppurativa

Drug Warnings

Withdrawn
gastrointestinal toxicity
Reports of adverse reactions and toxicity such as buccal ulceration, stomatitis, kerato-conjunctivitis. Studies have shown methylrosanilinium chloride to be a carcinogen in mice and it has been labell...
Country: Malaysia   Year: 1998
Withdrawn
carcinogenicity
Reports of adverse reactions and toxicity such as buccal ulceration, stomatitis, kerato-conjunctivitis. Studies have shown methylrosanilinium chloride to be a carcinogen in mice and it has been labell...
Country: Malaysia   Year: 1998
Withdrawn
gastrointestinal toxicity
Reports of adverse reactions and toxicity such as buccal ulceration, stomatitis, kerato-conjunctivitis. Studies have shown methylrosanilinium chloride to be a carcinogen in mice and it has been labell...
Country: Malaysia   Year: 1998
Withdrawn
occular toxicity
Reports of adverse reactions and toxicity such as buccal ulceration, stomatitis, kerato-conjunctivitis. Studies have shown methylrosanilinium chloride to be a carcinogen in mice and it has been labell...
Country: Malaysia   Year: 1998

Activity Summary

IC50 61 meas. best 6.73
Ki 25 meas. best 6.85
EC50 2 meas. best 7.66
Kd 1 meas. best 6.08

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
EC50 7.66 7.215 22.1 2
Muscarinic acetylcholine receptor M4
CHEMBL1821
Ki 6.85 6.85 140.0 1
Unchecked
CHEMBL612545
IC50 6.73 6.1146 185.9 13
Alpha-2A adrenergic receptor
CHEMBL1867
Ki 6.7 6.7 201.0 1
Muscarinic acetylcholine receptor M1
CHEMBL216
Ki 6.58 6.58 264.0 1
Alpha-2C adrenergic receptor
CHEMBL1916
Ki 6.56 6.56 274.0 1
D(3) dopamine receptor
CHEMBL234
Ki 6.55 6.55 282.0 1
Deoxyribonuclease-1
CHEMBL3351219
IC50 6.46 6.46 350.0 1
Muscarinic acetylcholine receptor M5
CHEMBL2035
Ki 6.42 6.42 384.0 1
HeLa
CHEMBL399
IC50 6.4 6.4 400.0 1
Unchecked
CHEMBL612545
Ki 6.38 5.9033 419.0 3
Epidermal growth factor receptor
CHEMBL203
IC50 6.33 6.33 473.0 1
Muscarinic acetylcholine receptor M2
CHEMBL211
Ki 6.29 6.29 508.0 1
Alpha-2A adrenergic receptor
CHEMBL1867
IC50 6.27 6.27 536.0 1
Muscarinic acetylcholine receptor M5
CHEMBL2035
IC50 6.27 6.27 535.0 1
Substance-K receptor
CHEMBL2327
Ki 6.25 6.25 560.0 1
Alpha-2B adrenergic receptor
CHEMBL1942
Ki 6.24 6.24 574.0 1
Kappa-type opioid receptor
CHEMBL237
Ki 6.21 6.21 616.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.12 6.12 751.0 1
Cytochrome P450 2D6
CHEMBL289
IC50 6.08 6.08 824.4 1
D(3) dopamine receptor
CHEMBL234
IC50 6.08 6.08 831.0 1
Unchecked
CHEMBL612545
Kd 6.08 6.08 830.0 1
Mu-type opioid receptor
CHEMBL233
Ki 6.06 6.06 871.0 1
Muscarinic acetylcholine receptor M3
CHEMBL245
Ki 6.04 6.04 918.0 1
Histone deacetylase 6
CHEMBL1865
IC50 6.02 6.02 953.2 1
Alpha-1D adrenergic receptor
CHEMBL223
Ki 6.01 6.01 973.0 1
Muscarinic acetylcholine receptor M4
CHEMBL1821
IC50 6.0 6.0 1005.0 1
D(2) dopamine receptor
CHEMBL217
Ki 5.97 5.97 1059.0 1
RAW264.7
CHEMBL612557
IC50 5.96 5.96 1100.0 1
Muscarinic acetylcholine receptor M1
CHEMBL216
IC50 5.96 5.96 1095.0 1
Histamine H2 receptor
CHEMBL1941
Ki 5.95 5.95 1136.0 1
Histamine H2 receptor
CHEMBL1941
IC50 5.94 5.94 1155.0 1
Alpha-2B adrenergic receptor
CHEMBL1942
IC50 5.9 5.9 1258.0 1
SK-MEL-2
CHEMBL614917
IC50 5.87 5.705 1360.0 2
Muscarinic acetylcholine receptor M2
CHEMBL211
IC50 5.84 5.84 1430.0 1
Kappa-type opioid receptor
CHEMBL237
IC50 5.81 5.81 1540.0 1
D(1A) dopamine receptor
CHEMBL2056
Ki 5.81 5.81 1551.0 1
Substance-K receptor
CHEMBL2327
IC50 5.78 5.78 1679.0 1
Alpha-2C adrenergic receptor
CHEMBL1916
IC50 5.72 5.72 1884.0 1
Adenosine receptor A2a
CHEMBL251
Ki 5.72 5.72 1889.0 1
Alpha-1D adrenergic receptor
CHEMBL223
IC50 5.7 5.7 1980.0 1
Alpha-1B adrenergic receptor
CHEMBL315
Ki 5.7 5.7 1990.0 1
Trypanosoma cruzi
CHEMBL368
IC50 5.68 4.965 2100.0 4
Tyrosine-protein kinase Fyn
CHEMBL1841
IC50 5.67 5.67 2148.0 1
Mu-type opioid receptor
CHEMBL233
IC50 5.67 5.67 2145.0 1
Adenosine receptor A3
CHEMBL256
Ki 5.63 5.63 2355.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
IC50 5.58 5.58 2627.0 1
D(1A) dopamine receptor
CHEMBL2056
IC50 5.51 5.51 3102.0 1
D(2) dopamine receptor
CHEMBL217
IC50 5.5 5.5 3178.0 1
Sodium-dependent dopamine transporter
CHEMBL238
Ki 5.49 5.49 3233.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmodium falciparum EC50 = 22.13 nM 7.66 NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferati... 18579783
Muscarinic acetylcholine receptor M4 Ki = 140.0 nM 6.85 DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Plasmodium falciparum EC50 = 170.3 nM 6.77 NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation ... 18579783
Unchecked IC50 = 185.9 nM 6.73 PubChem BioAssay. VEGF stimulated ADSC/ECFC co-culture CD31-stained tube area de... -
Alpha-2A adrenergic receptor Ki = 201.0 nM 6.7 DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912) -
Muscarinic acetylcholine receptor M1 Ki = 264.0 nM 6.58 DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Alpha-2C adrenergic receptor Ki = 274.0 nM 6.56 DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912) -
D(3) dopamine receptor Ki = 282.0 nM 6.55 DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone) -
Deoxyribonuclease-1 IC50 = 350.0 nM 6.46 Inhibition of DNase 1 (unknown origin) using (FAM)-labeled dsDNA as substrate 25042005
Muscarinic acetylcholine receptor M5 Ki = 384.0 nM 6.42 DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Unchecked IC50 = 393.9 nM 6.41 PubChem BioAssay. SNU-C1 viability from Cell TiterGlo-IC50. (Class of assay: c... -
HeLa IC50 = 400.0 nM 6.4 Antiproliferative activity against human HeLa cells 30108998
Unchecked Ki = 419.0 nM 6.38 DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotox... -
Unchecked IC50 = 460.0 nM 6.34 DRUGMATRIX: Sodium Channel, Site 2 radioligand binding (ligand: [3H] Batrachotox... -
Unchecked IC50 = 470.6 nM 6.33 PubChem BioAssay. DLD-1 viability from Cell TiterGlo-IC50. (Class of assay: co... -
Epidermal growth factor receptor IC50 = 473.0 nM 6.33 DRUGMATRIX: Protein Tyrosine Kinase, EGF Receptor enzyme inhibition (substrate: ... -
Unchecked IC50 = 466.5 nM 6.33 PubChem BioAssay. HT-29 viability from Cell TiterGlo-IC50. (Class of assay: co... -
Unchecked IC50 = 513.7 nM 6.29 PubChem BioAssay. HCT116 viability from Cell TiterGlo-IC50. (Class of assay: c... -
Muscarinic acetylcholine receptor M2 Ki = 508.0 nM 6.29 DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) -
Unchecked IC50 = 528.1 nM 6.28 PubChem BioAssay. SW480 viability from Cell TiterGlo-IC50. (Class of assay: co... -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3885881 Rattus norvegicus 430
20660673 10.1128/aac.01065-09 Staphylococcus aureus 10
28927904 10.1016/j.bmc.2017.08.021 Unchecked 9
18725450 10.1128/aac.00245-08 Pasteurella multocida 7
17548499 10.1128/aac.00339-07 Escherichia coli 7
18694955 10.1128/aac.00661-08 NON-PROTEIN TARGET 7
17638702 10.1128/aac.00072-07 Enterobacter cloacae 6
17055730 10.1016/j.bmc.2006.09.048 Trypanosoma cruzi 5
30852084 10.1016/j.bmcl.2019.02.028 Unchecked 5
20038628 10.1128/aac.01126-09 Escherichia coli 5
17325226 10.1128/aac.00182-07 Candida albicans 4
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
30852084 10.1016/j.bmcl.2019.02.028 GroEL/GroES 4
19884363 10.1128/aac.01168-09 Escherichia coli 4
- 10.6019/CHEMBL4808148 Histone deacetylase 6 4
17210767 10.1128/aac.01048-06 Escherichia coli 3
20014752 10.1021/tx900326k Hepatotoxicity 3
18591276 10.1128/aac.00475-08 Escherichia coli 3
25238291 10.1016/j.ejmech.2014.09.027 Trypanosoma cruzi 2
36961300 10.1021/acs.jmedchem.3c00094 Unchecked 2

Data from ChEMBL 36 via Core Engine