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Compound Detail

CHEMBL295124

BERBERINE
💊 Approved Drug
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💊 Approved Drug
COc1ccc2cc3[n+](cc2c1OC)CCc1cc2c(cc1-3)OCO2

Basic Information

ChEMBL ID CHEMBL295124
Name BERBERINE
Phase Approved
Structure Type MOL
InChI Key YBHILYKTIRIUTE-UHFFFAOYSA-N

Known Names

Berbericine Berberin Berberine Berberone Majarine Thalsine Umbellatin Umbellatine
36
Targets
78
Activities
4
Assay Types
8
PK Parameters
20
Publications
8
Known Names
6
Indications

Molecular Properties

336.4
MW (Da)
3.10
ALogP
4
HBA
0
HBD
40.8
PSA (Ų)
0.67
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Withdrawn
Chirality Achiral

Flags

Withdrawn Natural Product

Extended Properties

Molecular Formula C20H18NO4+
MW 336.37
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness 1.30

Indications

Diabetes Mellitus, Type 2 Hyperlipidemia, Familial Combined Adenocarcinoma of Lung Adenoma Non-alcoholic Fatty Liver Disease Prediabetic State

Drug Warnings

Withdrawn
hepatotoxicity
Jaundice, haemolytic anemia and kernicterus with brain damage in infants with glucose 6-phosphate dehydrogenase deficiency who were exposed either in utero or post-natally
Country: Singapore   Year: 1978
Withdrawn
neurotoxicity
Jaundice, haemolytic anemia and kernicterus with brain damage in infants with glucose 6-phosphate dehydrogenase deficiency who were exposed either in utero or post-natally
Country: Singapore   Year: 1978
Withdrawn
hematological toxicity
Jaundice, haemolytic anemia and kernicterus with brain damage in infants with glucose 6-phosphate dehydrogenase deficiency who were exposed either in utero or post-natally
Country: Singapore   Year: 1978

Activity Summary

IC50 45 meas. best 7.52
EC50 15 meas. best 7.0
Kd 11 meas. best 5.78
Ki 7 meas. best 7.36

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tryptophan 2,3-dioxygenase
CHEMBL2140
IC50 7.52 7.52 30.0 1
Cytochrome P450 1B1
CHEMBL4878
Ki 7.36 7.36 44.0 1
Cytochrome P450 1B1
CHEMBL4878
IC50 7.03 6.37 94.0 3
Acetylcholinesterase
CHEMBL220
IC50 7.0 6.3467 100.0 3
dsDNA
CHEMBL3832741
EC50 7.0 6.54 100.0 9
Indoleamine 2,3-dioxygenase 1
CHEMBL4685
IC50 6.58 6.58 260.0 1
Acetylcholinesterase
CHEMBL4078
IC50 6.43 6.22 374.0 3
Unchecked
CHEMBL612545
Ki 6.4 5.6775 400.0 4
Peroxisome proliferator-activated receptor alpha
CHEMBL239
EC50 6.24 6.24 580.0 1
Peroxisome proliferator-activated receptor alpha
CHEMBL239
Ki 6.14 6.14 730.0 1
Cholinesterase
CHEMBL1914
IC50 5.96 5.235 1090.0 2
quadruplex DNA
CHEMBL3832742
Kd 5.78 5.4011 1670.0 9
Chikungunya virus
CHEMBL4296563
EC50 5.75 5.735 1800.0 2
Unchecked
CHEMBL612545
Kd 5.75 5.75 1770.0 1
LNCaP
CHEMBL612518
IC50 5.47 5.47 3400.0 1
Aldo-keto reductase family 1 member C3
CHEMBL4681
IC50 5.39 5.31 4080.0 2
Aldo-keto reductase family 1 member C2
CHEMBL5847
IC50 5.17 5.17 6710.0 1
RAW264.7
CHEMBL612557
IC50 5.16 5.16 6900.0 1
Lysine-specific histone demethylase 1A
CHEMBL6136
IC50 5.16 5.16 6970.0 1
Hepatitis C virus
CHEMBL379
EC50 5.1 5.1 7870.0 2
Cholinesterase
CHEMBL5763
IC50 5.03 4.8367 9400.0 3
Cell division protein FtsZ
CHEMBL5096
IC50 5.0 5.0 10000.0 1
Unchecked
CHEMBL612545
IC50 5.0 4.89 10000.0 3
LNCaP C4-2B
CHEMBL4296461
IC50 4.95 4.95 11200.0 1
5'-AMP-activated protein kinase catalytic subunit alpha-2
CHEMBL2116
IC50 4.92 4.92 12000.0 1
CWR22R
CHEMBL612657
IC50 4.9 4.9 12700.0 1
Peroxisome proliferator-activated receptor delta
CHEMBL3979
EC50 4.85 4.85 14000.0 1
Neuraminidase
CHEMBL2051
Ki 4.84 4.84 14300.0 1
SW1990
CHEMBL1075592
IC50 4.74 4.74 18340.0 1
SMMC-7721
CHEMBL613831
IC50 4.74 4.74 18340.0 1
HUVEC
CHEMBL613979
IC50 4.74 4.74 18340.0 1
PC-3
CHEMBL390
IC50 4.67 4.67 21500.0 1
3T3-L1
CHEMBL614510
IC50 4.66 4.66 21840.0 1
Neuraminidase
CHEMBL3559643
IC50 4.49 4.455 32200.0 2
Telomerase reverse transcriptase
CHEMBL2916
IC50 4.43 4.43 37000.0 1
Zika virus
CHEMBL4296612
IC50 4.41 4.41 39100.0 1
HeLa 229
CHEMBL4483246
IC50 4.37 4.37 42930.0 1
Interleukin-8
CHEMBL2157
IC50 4.3 4.3 50000.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.18 4.18 66069.3 1
Tyrosine-protein phosphatase non-receptor type 1
CHEMBL335
IC50 4.17 4.17 67000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 24.18 ng.hr.mL-1 Rattus norvegicus
Cmax 20186.1 nM Rattus norvegicus
F 1.0 % Mus musculus
F 0.36 % Rattus norvegicus
Ka 0.65 10'-6/M Not specified
Ka 1.1 10'-5/M Homo sapiens
T1/2 7.88 hr Rattus norvegicus
Tmax 2.0 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tryptophan 2,3-dioxygenase IC50 = 30.0 nM 7.52 Inhibition of TDO (unknown origin) 39276584
Cytochrome P450 1B1 Ki = 44.0 nM 7.36 Inhibition of human CYP1B1 expressed in Escherichia coli DH5alpha coexpressing h... 28458135
Cytochrome P450 1B1 IC50 = 94.0 nM 7.03 Inhibition of human CYP1B1 expressed in Escherichia coli DH5alpha cell membranes... 30503941
Acetylcholinesterase IC50 = 100.0 nM 7.0 Inhibition of AChE (unknown origin) using acetylthiocholine as substrate assesse... 26003344
dsDNA EC50 = 100.0 nM 7.0 Binding affinity to double stranded DNA ssab2 (unknown origin) incubated for 0.5... 39213483
dsDNA EC50 = 130.0 nM 6.89 Binding affinity to double stranded DNA AT12 (unknown origin) incubated for 0.5 ... 39213483
dsDNA EC50 = 150.0 nM 6.82 Binding affinity to double stranded DNA AT15-2AT (unknown origin) incubated for ... 39213483
dsDNA EC50 = 230.0 nM 6.64 Binding affinity to double stranded DNA ssab3 (unknown origin) incubated for 0.5... 39213483
dsDNA EC50 = 230.0 nM 6.64 Binding affinity to double stranded DNA AT15-4AT (unknown origin) incubated for ... 39213483
Indoleamine 2,3-dioxygenase 1 IC50 = 260.0 nM 6.58 Inhibition of IDO1 (unknown origin) 39276584
Cytochrome P450 1B1 IC50 = 330.0 nM 6.48 Inhibition of human CYP1B1 expressed in Escherichia coli DH5alpha coexpressing h... 28458135
Acetylcholinesterase IC50 = 374.0 nM 6.43 Inhibition of electric eel AChE using acetylthiocholine chloride substrate as su... 22019228
Acetylcholinesterase IC50 = 374.0 nM 6.43 Inhibition of electric eel AChE using acetylcholine as substrate by Ellman's met... 22472046
Unchecked Ki = 400.0 nM 6.4 Binding affinity to poly(A) tail mRNA (unknown origin) assessed as apparent bind... -
dsDNA EC50 = 400.0 nM 6.4 Binding affinity to double stranded DNA AT15-6AT (unknown origin) incubated for ... 39213483
Unchecked Ki = 410.0 nM 6.39 Binding affinity to poly(A) tail mRNA (unknown origin) assessed as apparent bind... -
dsDNA EC50 = 450.0 nM 6.35 Binding affinity to double stranded DNA ssab1 (unknown origin) incubated for 0.5... 39213483
Peroxisome proliferator-activated receptor alpha EC50 = 580.0 nM 6.24 Agonist activity at PPARalpha (unknown origin) 33992930
Acetylcholinesterase IC50 = 700.0 nM 6.16 Inhibition of human AChE using acetylthiocholine iodide as substrate measured fo... 30701972
Peroxisome proliferator-activated receptor alpha Ki = 730.0 nM 6.14 Binding affinity to PPARalpha (unknown origin) 33992930

Literature References

Data from ChEMBL 36 via Core Engine