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Compound Detail

CHEMBL294199

CAPSAICIN
💊 Approved Drug
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💊 Approved Drug
COc1cc(CNC(=O)CCCC/C=C/C(C)C)ccc1O

Basic Information

ChEMBL ID CHEMBL294199
Name CAPSAICIN
Phase Approved
Structure Type MOL
InChI Key YKPUWZUDDOIDPM-SOFGYWHQSA-N
Therapeutic ✓ Yes

Known Names

ALGRX 4975 ALGRX-4975 Ausanil Axsain Capsaicin Capsaicina Capsaicine Capzasin-hp Cntx-4975 Dolenon FEMA NO. 3404 Mioton +11 more
24
Targets
76
Activities
3
Assay Types
1
PK Parameters
20
Publications
23
Known Names
20
Indications
1
Mechanisms

Molecular Properties

305.4
MW (Da)
3.79
ALogP
3
HBA
2
HBD
58.6
PSA (Ų)
0.54
QED
0
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2009
Availability Prescription
Chirality Achiral

Routes of Administration

Topical

Flags

Natural Product

Extended Properties

Molecular Formula C18H27NO3
MW 305.42
Aromatic Rings 1
Heavy Atoms 22
NP-Likeness 0.54

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Vanilloid receptor opener OPENER Transient receptor potential cation channel subfamily V member 1

Indications

Arthralgia Arthritis Back Pain Bursitis Contusions Muscle Cramp Myalgia Neuralgia Neuralgia Osteoarthritis Pain Sprains and Strains Tendinopathy Angina, Stable Breast Neoplasms Common Cold Diabetic Neuropathies Diabetic Neuropathies Head and Neck Neoplasms Herpes Zoster

ATC Classification

M02AB01
capsaicin
Level 1: MUSCULO-SKELETAL SYSTEM
Level 2: TOPICAL PRODUCTS FOR JOINT AND MUSCULAR PAIN
N01BX04
capsaicin
Level 1: NERVOUS SYSTEM
Level 2: ANESTHETICS

Activity Summary

EC50 34 meas. best 8.6
IC50 31 meas. best 8.1
Ki 11 meas. best 8.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Transient receptor potential cation channel subfamily V member 1
CHEMBL4794
EC50 8.6 7.3724 2.5 17
Transient receptor potential cation channel subfamily V member 1
CHEMBL4794
Ki 8.22 6.4325 6.0 4
Transient receptor potential cation channel subfamily V member 1
CHEMBL4794
IC50 8.1 7.436 8.0 5
Transient receptor potential cation channel subfamily V member 1
CHEMBL5102
IC50 7.72 7.72 19.0 1
Vanilloid receptor
CHEMBL2096684
EC50 7.52 6.6867 30.0 6
Transient receptor potential cation channel subfamily V member 1
CHEMBL5102
EC50 7.35 6.92 44.8 4
Cavia porcellus
CHEMBL369
EC50 6.58 6.58 260.0 3
Rattus norvegicus
CHEMBL376
EC50 6.52 6.52 300.0 2
Lysine-specific histone demethylase 1A
CHEMBL6136
IC50 6.22 6.22 600.0 4
Transient receptor potential cation channel subfamily M member 8
CHEMBL1075319
IC50 6.0 6.0 1000.0 1
Prostaglandin G/H synthase 1
CHEMBL221
IC50 5.81 5.615 1551.0 2
Transient receptor potential cation channel subfamily V member 1
CHEMBL5102
Ki 5.77 5.7333 1700.0 6
Cytochrome P450 1A2
CHEMBL3356
IC50 5.52 5.52 3000.0 1
BGC-823
CHEMBL614526
IC50 5.33 5.33 4659.0 1
SH-SY5Y
CHEMBL614910
EC50 4.85 4.85 14020.0 1
Unchecked
CHEMBL612545
EC50 4.79 4.79 16370.0 1
Unchecked
CHEMBL612545
IC50 4.77 4.77 16982.4 1
SK-OV-3
CHEMBL614925
IC50 4.66 4.66 22030.0 1
Transient receptor potential cation channel subfamily M member 8
CHEMBL3108632
IC50 4.55 4.55 28000.0 1
Potassium voltage-gated channel subfamily A member 1
CHEMBL2309
IC50 4.54 4.54 29000.0 1
NCI-H460
CHEMBL396
IC50 4.51 4.51 30660.0 1
HCT-116
CHEMBL394
IC50 4.4 4.4 40160.0 1
Tyrosine--tRNA ligase, cytoplasmic
CHEMBL3179
Ki 4.38 4.38 42000.0 1
K562
CHEMBL385
IC50 4.31 4.31 49410.0 1
MCF7
CHEMBL387
IC50 4.3 4.15 49970.0 2
No relevant target
CHEMBL2362975
IC50 4.3 4.3 50300.0 1
NADH-ubiquinone oxidoreductase chain 1
CHEMBL4497
IC50 4.28 4.28 52480.8 1
Polyunsaturated fatty acid 5-lipoxygenase
CHEMBL215
IC50 4.25 4.25 56000.0 1
T47D
CHEMBL614361
IC50 4.0 4.0 100000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 212.0 mL.min-1.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Transient receptor potential cation channel subfamily V member 1 EC50 = 2.512 nM 8.6 Agonist activity at human TRPV1 expressed in tetracycline-stimulated HEK293 cell... 20381363
Transient receptor potential cation channel subfamily V member 1 EC50 = 3.9 nM 8.41 Agonist activity at human TRPV1 ion channel expressed in HEK293 cells assessed a... 22257892
Transient receptor potential cation channel subfamily V member 1 EC50 = 5.0 nM 8.3 Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed a... 37192374
Transient receptor potential cation channel subfamily V member 1 EC50 = 5.3 nM 8.28 Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed a... 25666822
Transient receptor potential cation channel subfamily V member 1 EC50 = 5.3 nM 8.28 Agonist activity at human TRPV1 stably transfected in HEK293 cells assessed as i... 33136399
Transient receptor potential cation channel subfamily V member 1 Ki = 6.0 nM 8.22 Binding affinity to human recombinant TRPV1 20947352
Transient receptor potential cation channel subfamily V member 1 EC50 = 7.2 nM 8.14 Agonist activity at human TRPV1 expressed in HEK293T cells assessed as increase ... 31104785
Transient receptor potential cation channel subfamily V member 1 IC50 = 8.0 nM 8.1 Antagonist activity at human TRPV1 stably transfected in HEK293 cells assessed a... 33136399
Transient receptor potential cation channel subfamily V member 1 IC50 = 8.0 nM 8.1 Antagonist activity at human recombinant TRPV1 expressed in HEK293 cells assesse... 37192374
Transient receptor potential cation channel subfamily V member 1 IC50 = 8.0 nM 8.1 Antagonist activity against human recombinant TRPV1 expressed in HEK293 cells as... 25666822
Transient receptor potential cation channel subfamily V member 1 IC50 = 19.0 nM 7.72 Binding affinity to rat TRPV1 20947352
Transient receptor potential cation channel subfamily V member 1 EC50 = 20.0 nM 7.7 Agonist activity at human recombinant TRPV1 expressed in HEK293 cells assessed a... 19361197
Transient receptor potential cation channel subfamily V member 1 EC50 = 19.95 nM 7.7 Concentration necessary to induce a relative half-maximal response measured by t... 12166946
Transient receptor potential cation channel subfamily V member 1 EC50 = 25.9 nM 7.59 Agonist activity at human TRPV1 expressed in CHO cells assessed as increase in 4... 31702924
Transient receptor potential cation channel subfamily V member 1 EC50 = 29.0 nM 7.54 Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase i... 36008373
Vanilloid receptor EC50 = 30.0 nM 7.52 In vitro agonist activity, increased [Ca2+] influx, at vanilloid receptor of rat... 14741290
Transient receptor potential cation channel subfamily V member 1 EC50 = 40.0 nM 7.4 Agonist activity at human recombinant TRPV1 expressed in human HEK293 cells 17046253
Transient receptor potential cation channel subfamily V member 1 EC50 = 40.0 nM 7.4 Agonist activity at human TRPV1 expressed in HEK293 cells assessed as increase i... 19951840
Transient receptor potential cation channel subfamily V member 1 EC50 = 44.8 nM 7.35 Agonist activity at human TRPV1 expressed in CHO cells assessed as stimulation o... 33385210
Transient receptor potential cation channel subfamily V member 1 EC50 = 44.8 nM 7.35 Agonist activity at rat TRPV1 expressed in CHO cells assessed as increase in 45C... 31702924

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3885881 Rattus norvegicus 270
29543451 10.1021/acs.jmedchem.8b00156 Transient receptor potential cation channel subfamily V member 1 13
32945672 10.1021/acs.jmedchem.0c00958 Lipid bilayer 7
31702924 10.1021/acs.jmedchem.9b01046 Transient receptor potential cation channel subfamily V member 1 6
31702924 10.1021/acs.jmedchem.9b01046 ADMET 6
24484240 10.1021/np400885u Transient receptor potential cation channel subfamily M member 8 5
29722529 10.1021/acs.jmedchem.8b00109 ADMET 5
8573592 10.1016/0005-2728(95)00131-x Unchecked 4
12825950 10.1021/jm030089u Transient receptor potential cation channel subfamily V member 1 4
27159637 10.1021/acs.jnatprod.5b00599 Transient receptor potential cation channel subfamily V member 1 4
20014752 10.1021/tx900326k Hepatotoxicity 3
36510819 10.1021/acs.jmedchem.2c01604 Staphylococcus aureus 3
- 10.1007/s00044-008-9122-3 Acetylcholinesterase 3
25666822 10.1016/j.bmcl.2015.01.039 Transient receptor potential cation channel subfamily V member 1 3
8960554 10.1021/jm960512h Mus musculus 3
33136399 10.1021/acs.jnatprod.0c00639 Transient receptor potential cation channel subfamily V member 1 3
36008373 10.1021/acs.jmedchem.2c00469 Transient receptor potential cation channel subfamily V member 1 3
19135377 10.1016/j.bmc.2008.11.085 Transient receptor potential cation channel subfamily V member 1 3
36008373 10.1021/acs.jmedchem.2c00469 ADMET 3
34795858 10.1021/acsmedchemlett.1c00304 NCI-H460 3

Data from ChEMBL 36 via Core Engine