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Compound Detail

CHEMBL1200494

GUANFACINE HYDROCHLORIDE
💊 Approved Drug
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💊 Approved Drug
Cl.N=C(N)NC(=O)Cc1c(Cl)cccc1Cl
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1200494
Name GUANFACINE HYDROCHLORIDE
Phase Approved
Structure Type MOL
InChI Key DGFYECXYGUIODH-UHFFFAOYSA-N
Therapeutic ✓ Yes
Parent Compound CHEMBL862
Active Moiety CHEMBL862

Known Names

Akfen BS 100-141 BS-100-141 Estulic Guafacine hydrochloride Guanfacine hcl Guanfacine hydrochloride Intuniv SPD503 Tenex
2
Targets
7
Activities
2
Assay Types
0
PK Parameters
20
Publications
10
Known Names
2
Indications
1
Mechanisms

Molecular Properties

246.1
MW (Da)
1.55
ALogP
2
HBA
3
HBD
79.0
PSA (Ų)
0.55
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1986
Availability Prescription
Chirality Achiral

Routes of Administration

Oral
USAN Stem guan-
USAN Year 1979

Extended Properties

Molecular Formula C9H10Cl3N3O
MW 282.56
Aromatic Rings 1
Heavy Atoms 15
NP-Likeness -1.12

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Adrenergic receptor alpha-2 agonist AGONIST Adrenergic receptor alpha-2 ✓ ✓

Indications

Attention Deficit Disorder with Hyperactivity Hypertension

Activity Summary

IC50 6 meas. best 5.9
EC50 1 meas. best 7.93

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-2A adrenergic receptor
CHEMBL1867
 EC50 7.93 7.93 11.8 1
Plasmodium falciparum
CHEMBL364
 IC50 5.9 5.5167 1258.9 6

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Alpha-2A adrenergic receptor EC50 = 11.77 nM 7.93 GPCR PRESTO-Tango dose-response in agonist mode with target: ADRA2A -
Plasmodium falciparum IC50 = 1258.93 nM 5.9 Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 2511.89 nM 5.6 Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr... 19734910
Plasmodium falciparum IC50 = 3162.28 nM 5.5 Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 3981.07 nM 5.4 Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 3981.07 nM 5.4 Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 5011.87 nM 5.3 Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR g... 19734910

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5724801 Fibroblast 304
- 10.6019/CHEMBL5724801 HEK-293T 304
- 10.6019/CHEMBL5724801 U2OS 304
- 10.6019/CHEMBL5058577 HEK-293T 304
- 10.6019/CHEMBL5058577 U2OS 304
- 10.6019/CHEMBL5058577 Fibroblast 304
19734910 10.1038/nchembio.215 Plasmodium falciparum 6
- 10.6019/CHEMBL5058564 Fibroblast 6
- 10.6019/CHEMBL5058564 HEK-293T 5
- 10.6019/CHEMBL5209801 Apelin receptor 2
- 10.6019/CHEMBL5209801 Free fatty acid receptor 4 2
- 10.6019/CHEMBL5209801 CX3C chemokine receptor 1 2
- 10.6019/CHEMBL5209801 G-protein coupled receptor 35 2
- 10.6019/CHEMBL5209801 Beta-2 adrenergic receptor 2
- 10.6019/CHEMBL5209801 Glucose-dependent insulinotropic receptor 2
- 10.6019/CHEMBL5209801 Type-1 angiotensin II receptor 2
- 10.6019/CHEMBL5058564 U2OS 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
- 10.6019/CHEMBL5209801 Adhesion G-protein coupled receptor F1 2
- 10.6019/CHEMBL5209801 Glucagon-like peptide 1 receptor 2

Data from ChEMBL 36 via Core Engine