Table 1.
Significant hits from the MBD2_MBD TR FRET binding assay applied to the Sigma® LOPAC™ screen
| Compound* | Primary Screen P- Value |
MBD2-MBD Secondary Screen IC50 |
SP-1 Counterscreen IC50 |
Description |
|---|---|---|---|---|
| 6-Hydroxy-DL-DOPA | 2.16E-07 | >50µM | Not Assayed | Precursor of the catecholaminergic neurotoxin, 6- hydroxydopamine; converted to 6-hydroxydopamine by L-aromatic amino acid decarboxylase.1 |
| Aurintricarboxylic acid | 2.56E-07 | 2.7nM | <lnm | DNA topoisomerase II inhibitor. Polymerizes in water.1 |
| Dephostatin | 5.50E-07 | >50µM | Not Assayed | CD45 protein tyrosine kinase inhibitor.1 |
| NF449 octasodium salt | 7.08E-07 | 290nM | 24.7nM | Potent G protein antagonist, selective for Gs-alpha1. P2X1 selective protein inhibitor.2 |
| Idarubicin | 7.90E-07 | 196nM | 580nM | Antineoplastic1. DNA intercalator. |
| Reactive Blue 2 | 1.67E-06 | Not Assayed | Not Assayed | P2Y receptor antagonist; most potent antagonist for ATP activated channels.1 |
| Me-3,4-dephostatin | 1.74E-06 | >50µM | Not Assayed | Selective inhibitor of protein tyrosine phosphatase IB and SHPTP-1.1 |
| Carbetapentane citrate | 5.19E-06 | >50µM | Not Assayed | Opioid receptor ligand with high affinity toward sigma1 sites; antitussive.1 |
| (2S,1S,2S)-2- (carboxycyclopropyl)glycine L- CCG-I |
5.69E-06 | >50µM | Not Assayed | Potent group II metabotropicglutamate receptor agonist.1 |
| Mitoxantrone | 1.72E-05 | 94nM | 314nM | DNA synthesis inhibitor1. DNA intercalator. |
1
Sigma Aldrich Website, (http://www.sigmaaldrich.com/chemistry/drug-discovery/validation-libraries/lopac1280-navigator.html)
2
El-Ajouz, S., et al, Molecular basis of selective antagonism of the P2X1 receptor for ATP by NF449 and suramin: contribution of basic amino acids in the cysteine-rich loop. Br J Pharmacol, 2012. 165(2): p. 390–400. (Ref. 21).