2-APB

Ligand id: 2433

Name: 2-APB

Structure and Physico-chemical Properties

2D Structure
Calculated Physico-chemical Properties
Hydrogen bond acceptors 2
Hydrogen bond donors 1
Rotatable bonds 5
Topological polar surface area 35.25
Molecular weight 225.13
XLogP 4.46
No. Lipinski's rules broken 0

Molecular properties generated using the CDK

View interactive charts of activity data from GtoPdb and ChEMBL (where available) across species

Selectivity at ion channels
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Affinity Units Concentration range (M) Reference
TRPM7 Mm Activator Activation - - > 1x10-3 7
Conc range: > 1x10-3 M [7]
TRPM3 Hs Gating inhibitor Antagonist - - 1x10-4 13
Conc range: 1x10-4 M [13]
Voltage: Physiological
TRPC2 Mm Channel blocker Antagonist - - 5x10-5 6
Conc range: 5x10-5 M [6]
Voltage: -70.0 – 80.0 mV
TRPV2 Rn Activator - 5.0 pEC50 - 9-10
pEC50 5.0 (EC50 1x10-5 M) [9-10]
TRPV3 Mm Activator Full agonist 4.6 pEC50 - 1
pEC50 4.6 (EC50 2.51x10-5 M) [1]
Voltage: -80.0 – 80.0 mV
Description: Patch clamp electrophysiology
TRPV2 Mm Activator Agonist 3.8 – 3.9 pEC50 - 2-3
pEC50 3.8 – 3.9 (EC50 1.6x10-4 – 1.29x10-4 M) [2-3]
Voltage: Physiological
TRPV1 Mm Activator Agonist 3.7 – 3.9 pEC50 - 2
pEC50 3.7 – 3.9 [2]
Voltage: -40.0 mV
TRPM6 Hs Activator Agonist 3.4 – 3.7 pEC50 - 4
pEC50 3.4 – 3.7 (EC50 3.8x10-4 – 2.05x10-4 M) Potentiation [4]
Voltage: -120.0 – 100.0 mV
TRPM2 Hs Channel blocker Antagonist 6.1 pIC50 - 12
pIC50 6.1 (IC50 8.2x10-7 M) [12]
Voltage: -60.0 mV
TRPC3 Hs Channel blocker Antagonist 5.0 pIC50 - 5
pIC50 5.0 (IC50 1x10-5 M) [5]
Voltage: Physiological
TRPM8 Mm Channel blocker Antagonist 4.9 – 5.1 pIC50 - 2,8
pIC50 4.9 – 5.1 [2,8]
Voltage: 100.0 – -100.0 mV
TRPC5 Hs Channel blocker Antagonist 4.7 pIC50 - 13
pIC50 4.7 (IC50 2x10-5 M) [13]
Voltage: -80.0 mV
TRPM7 Mm Channel blocker Inhibition 3.8 pIC50 - 4
pIC50 3.8 (IC50 1.78x10-4 M) Reversible inhibition [4]
Voltage: -100.0 – 100.0 mV
TRPC1 Hs Channel blocker Antagonist - - - 11
[11]
Voltage: -70.0 mV
TRPC4 Hs Channel blocker - - - -
TRPC6 Hs Channel blocker - - - -
TRPC7 Hs Channel blocker - - - -
TRPV1 Hs Channel blocker - - - -
TRPV6 Hs Activator Potentiation - - -
Targets where the ligand is described in the comment field
Target Comment
Ligand mentioned in the following text fields