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Compound Detail

CHEMBL1617

RIFAXIMIN
💊 Approved Drug
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💊 Approved Drug
CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(c5c(nc6cc(C)ccn65)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C

Basic Information

ChEMBL ID CHEMBL1617
Name RIFAXIMIN
Phase Approved
Structure Type MOL
InChI Key NZCRJKRKKOLAOJ-XRCRFVBUSA-N
Therapeutic ✓ Yes

Known Names

L-105 Normix NSC-758957 Rifacol Rifamycin l 105 Rifaxidin Rifaximin Rifaximina Rifaximine Targaxan Xifaxan Xifaxanta +1 more
5
Targets
9
Activities
2
Assay Types
7
PK Parameters
20
Publications
13
Known Names
20
Indications
1
Mechanisms

Molecular Properties

785.9
MW (Da)
6.16
ALogP
13
HBA
5
HBD
198.4
PSA (Ų)
0.11
QED
3
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 2004
Availability Prescription
Chirality Single Enantiomer

Routes of Administration

Oral

Flags

Natural Product
USAN Stem rifa-
USAN Year 1992

Extended Properties

Molecular Formula C43H51N3O11
MW 785.89
Aromatic Rings 4
Heavy Atoms 57
NP-Likeness 1.64

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Bacterial DNA-directed RNA polymerase inhibitor INHIBITOR Bacterial DNA-directed RNA polymerase

Indications

Diarrhea Hepatic Encephalopathy Infections Brain Diseases Clostridium Infections Colitis, Collagenous Crohn Disease Helicobacter Infections Hepatitis, Alcoholic Irritable Bowel Syndrome Liver Cirrhosis Parkinson Disease Peritonitis Rectal Neoplasms Alzheimer Disease Anemia, Sickle Cell Breast Neoplasms Diverticulitis Dyspepsia Heart Failure, Systolic

ATC Classification

A07AA11
rifaximin
Level 1: ALIMENTARY TRACT AND METABOLISM
Level 2: ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
D06AX11
rifaximin
Level 1: DERMATOLOGICALS
Level 2: ANTIBIOTICS AND CHEMOTHERAPEUTICS FOR DERMATOLOGICAL USE

Activity Summary

EC50 5 meas. best 5.66
IC50 4 meas. best 4.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nuclear receptor subfamily 1 group I member 2
CHEMBL3401
EC50 5.66 5.142 2200.0 5
ATP-binding cassette sub-family C member 2
CHEMBL5748
IC50 4.81 4.81 15400.0 1
ATP-binding cassette sub-family C member 4
CHEMBL1743128
IC50 4.52 4.52 30200.0 1
Bile salt export pump
CHEMBL6020
IC50 4.38 4.38 42000.0 1
ATP-binding cassette sub-family C member 3
CHEMBL5918
IC50 4.19 4.19 65000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 6.95 ng.hr.mL-1 Homo sapiens
AUC 7.83 ng.hr.mL-1 Homo sapiens
Cmax 2.074 nM Homo sapiens
Cmax 1.565 nM Homo sapiens
F 0.4 % Homo sapiens
Tmax 2.77 hr Homo sapiens
Tmax 2.11 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18955526 10.1128/aac.00441-08 NON-PROTEIN TARGET 166
21599020 10.1021/jm200241s Mus musculus 18
19858255 10.1128/aac.00691-09 HEp-2 17
20547807 10.1128/aac.00161-10 Escherichia coli 17
22194678 10.1371/journal.pcbi.1002310 Hepatotoxicity 14
18195066 10.1128/aac.01143-07 Clostridioides difficile 12
17526759 10.1128/aac.01397-06 Escherichia coli 11
19114678 10.1128/aac.01260-08 NON-PROTEIN TARGET 11
15646539 10.1016/s0399-8320(04)95062-2 Unchecked 11
18086855 10.1128/aac.01108-07 Homo sapiens 9
19858255 10.1128/aac.00691-09 Escherichia coli 8
15646539 10.1016/s0399-8320(04)95062-2 NON-PROTEIN TARGET 8
20966043 10.1124/dmd.110.035105 Nuclear receptor subfamily 1 group I member 2 5
17606690 10.1128/aac.00343-07 Staphylococcus epidermidis 5
25455183 10.1016/j.bmcl.2014.09.081 No relevant target 4
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
18955526 10.1128/aac.00441-08 Clostridium tertium 3
18955526 10.1128/aac.00441-08 Clostridium sporogenes 3
18955526 10.1128/aac.00441-08 Paeniclostridium sordellii 3
18955526 10.1128/aac.00441-08 Lactobacillus acidophilus 3

Data from ChEMBL 36 via Core Engine