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Chemical probes are specific small molecules used in biological research to investigate the function and behavior of biomolecules within cells or organisms. These probes are designed to interact with their target molecules in a highly selective and often reversible manner, enabling researchers to modulate the activity of the target and study its biological effects. It is a gateway to understanding fundamental biological processes, aiding in developing first-in-class drugs.
Library of High-Potency Chemical Probes is a collection of 67 compounds designed to advance the field of drug discovery and biological research. This library stands out for the stringent selection criteria, focusing on compounds with exceptional potency (pX ≥ 7) and selectivity (≥ 1.5 pX), ensuring the highest level of precision in modulating biological targets. This precision makes them invaluable for complementing traditional target validation methods and disease pathology.
Related terms: chemical probes, DVL1, Estrogen receptor, Cav2.1, 5-HT2A receptor, GABAA receptor, V2 receptor, Ferroportin, H3 receptor.
UCSF4226 is a high affinity brain-penetrant inverse agonist of melatonin receptor MTNR1B (MT2)
TP-040 is an inhibitor of OGA with an IC50 value of 46 nM.
ML252 is a selective inhibitor of potassium channel , targeting to KCNQ2 channel (Kv7.2) (IC50 =69 nM).
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NoteAll the compounds with solubility below 10 mM are shipped as 2 mM solutions.
G protein-coupled receptors
25
25
Number of compounds
25
Receptor tyrosine kinases (RTKs)
15
15
Number of compounds
15
Non-receptor tyrosine kinases (nRTKs)
7
7
Number of compounds
7
Nuclear hormone receptors
7
7
Number of compounds
7
MA: Metallo (M) Peptidases
5
5
Number of compounds
5
Voltage-gated ion channels
4
4
Number of compounds
4
Ligand-gated ion channels
4
4
Number of compounds
4
Steroid hormone receptors
4
4
Number of compounds
4
Cyclin-dependent kinase (CDK) family
4
4
Number of compounds
4
Catalytic receptors
3
3
Number of compounds
3
Orphan and other 7TM receptors
3
3
Number of compounds
3
Eicosanoid turnover
3
3
Number of compounds
3
Tubulins
2
2
Number of compounds
2
SLC superfamily of solute carriers
2
2
Number of compounds
2
ATP-binding cassette transporter family
2
2
Number of compounds
2
Glycerophospholipid turnover
2
2
Number of compounds
2
CMGC: Containing CDK, MAPK, GSK3, CLK families
2
2
Number of compounds
2
Lipid modifying kinases
2
2
Number of compounds
2
Pattern recognition receptors
2
2
Number of compounds
2
SLC22 family of organic cation and anion transporters
2
2
Number of compounds
2
AA: Aspartic (A) Peptidases
2
2
Number of compounds
2
Cytochrome P450
2
2
Number of compounds
2
Oxidoreductases
2
2
Number of compounds
2
Ceramide turnover
2
2
Number of compounds
2
Dual-specificity tyrosine-(Y)-phosphorylation regulated kinase (DYRK) family
1
1
Number of compounds
1
Catecholamine turnover
1
1
Number of compounds
1
Poly ADP-ribose polymerases
1
1
Number of compounds
1
DNA topoisomerases
1
1
Number of compounds
1
MC: Metallo (M) Peptidases
1
1
Number of compounds
1
Chromatin modifying enzymes
1
1
Number of compounds
1
Mitogen-activated protein kinases (MAP kinases)
1
1
Number of compounds
1
Aryl hydrocarbon receptor complex
1
1
Number of compounds
1
RSK family
1
1
Number of compounds
1
Polo-like kinase (PLK) family
1
1
Number of compounds
1
SC: Serine (S) Peptidases
1
1
Number of compounds
1
Carrier proteins
1
1
Number of compounds
1
Glutaminases
1
1
Number of compounds
1
CAMK: Calcium/calmodulin-dependent protein kinases
1
1
Number of compounds
1
Chloride channels
1
1
Number of compounds
1
Cytokine receptor family
1
1
Number of compounds
1
Glycogen synthase kinase (GSK) family
1
1
Number of compounds
1
Sigma receptors
1
1
Number of compounds
1
Viral protein targets
1
1
Number of compounds
1
IKK family
1
1
Number of compounds
1
DMPK family
1
1
Number of compounds
1
Amino acid hydroxylases
1
1
Number of compounds
1
Endocannabinoid turnover
1
1
Number of compounds
1
MH: Metallo (M) Peptidases
1
1
Number of compounds
1
CAMKK family
1
1
Number of compounds
1
Acetylcholine turnover
1
1
Number of compounds
1
Adenosine turnover
1
1
Number of compounds
1
MG: Metallo (M) Peptidases
1
1
Number of compounds
1
CA: Cysteine (C) Peptidases
1
1
Number of compounds
1
B-cell lymphoma 2 (Bcl-2) protein family
1
1
Number of compounds
1
Potassium channels
1
1
Number of compounds
1
Inhibitors of apoptosis (IAP) protein family
1
1
Number of compounds
1
PA: Serine (S) Peptidases
1
1
Number of compounds
1
Membrane bound O-acyltransferases
1
1
Number of compounds
1
AGC: Containing PKA, PKG, PKC families
1
1
Number of compounds
1
Adiponectin receptors
1
1
Number of compounds
1
Aurora kinase (Aur) family
1
1
Number of compounds
1
Interleukin-1 receptor-associated kinase (IRAK) family
1
1
Number of compounds
1
Immunoglobulin like domain containing proteins
1
1
Number of compounds
1
SLC6 neurotransmitter transporter family
1
1
Number of compounds
1
TKL-unique family
1
1
Number of compounds
1
EBCL-0035