allosteric

MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4).

Refametinib (RDEA119) (RDEA119, Bay 86-9766) is an effective, ATP non-competitive and specific inhibitor of MEK1/2 (IC50: 19/47 nM).

Bithionol (Actamer), formerly marketed as an active ingredient in various topical drug products, was shown to be a potent photosensitizer with the potential to cause serious skin disorders. Approvals of the NDA's for bithionol drug products were withdrawn on October 24, 1967.

Adenosine A1 receptor activator T62 is an allosteric enhancer of the adenosine A1 receptor, producing antinociception in animal models of acute pain and reducing hypersensitivity in models of inflammatory and nerve-injury pain[1][2][3].

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.

TQS (4-Naphthalen-1-yl-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide) is a positive allosteric modulator of α7 nACh receptors.

CK-666 is a cell-permeable inhibitor of the actin-related protein Arp2/3 complex, binding to and stabilizing its inactive state, thereby preventing the movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) configuration.

TNO155 is a protein tyrosine phosphatase (PTP) non-receptor type 11 (SHP2; src homology region 2 domain phosphatase; PTPN11) inhibitor(IC50 : 0.011 µM),with potential antineoplastic activity.

(Z)-Leukadherin-1 (ADH-503 free base) is an allosteric agonist of CD11b.

Danicamtiv (MYK-491) is an inotropic agent and it also is a selective allosteric activator of cardiac myosin. Danicamtiv increases cardiac systolic function and preserves mechanical efficiency.

CX516 (Ampalex), an ampakine and nootropic, acts as an AMPA receptor positive allosteric modulator as a therapy for Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).

A 286982 is an inhibitor that blocks the integrin-ligand interaction between leukocyte function-associated antigen-1 (LFA-1) and intercellular adhesion molecule-1.

AH-7614 (AH 7614) is a selective and potent free fatty acid receptor 4 (FFA4/GPR120) antagonist.

Brr2-IN-3 (Brr2 Inhibitor C9) is an allosteric inhibitor of the spliceosomal RNA helicase Brr2. Brr2 is implicated in autosomal-dominant retinitis pigmentosa (a group of progressive retinal degenerative disorders).

CDPPB is a modulator of mGluR5 positive allosteric(with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5).

CYM-5520 is a noncompetitive allosteric agonist of S1P2

MMPIP hydrochloride is a selective antagonist of allosteric mGluR7. MMPIP hydrochloride can be used in research on the roles of mGluR7 on central nervous system functions.

VU10010 (VU 10010) is allosteric potentiator of M4 acetylcholine receptors.

VU-29 is a positive allosteric mGlu5 receptor modulator with an EC50 of 9 nM and a Ki of 244 nM for rmGluR5. It is selective for mGluR5 relative to other mGluR subtypes [EC50: rmGluR1/rmGluR2=557 nM/1.5 μM; hmGluR4=154 nM].

ML141 (CID-2950007) is an effective, specific and reversible non-competitive inhibitor of Rho family GTPase cdc42 (IC50: 200 nM).

6-Hydroxy-DOPA is an allosteric inhibitor of RAD52, it inhibits proliferation of BRCA-deficient cancer cells in vitro and also inhibits APE1.

BMS-986122 (BMS 986122) is a positive allosteric modulator of μ-opioid receptors that increases β-arrestin recruitment stimulated by endomorphin 1 in U2OS-OPRM1 human osteosarcoma cells expressing μ-opioid receptors (EC50 = 3 μM).

ML380 is a highly potent and the first CNS penetrant M5 positive allosteric modulator (PAM).

VU0453595 is a M1 positive allosteric modulator (PAM).