Examples of proposed allosteric modulator classifications

Target ClassTargetLigandProposed Ligand Descriptors
GPCRCannabinoid CB1 receptorOrg27569Org27569 is a PAM of CP55940 affinity but a NAM of CP55940 efficacy for mediating inhibition of cAMP accumulation.
GPCRmGlu1 receptorCPCCOEtCPCCOEt is a NAL with respect to glutamate affinity but a NAM of glutamate efficacy in mediating intracellular calcium mobilization
GPCRmGlu5 receptorM-5MPEPM-5MPEP is a NAL with respect to glutamate affinity and NAM of glutamate efficacy for stimulation of intracellular calcium mobilization and inositol phosphate accumulation
GPCRCCR5AplavirocAplaviroc is a NAM of CCL3 affinity and a NAL with respect to CCL5 affinity; it is also a NAM of CCL3 and CCL5 efficacy to stimulate intracellular calcium mobilization.
LGICBenzodiazepine-sensitive GABAA receptorsDiazepamDiazepam is a PAM of GABA affinity and chloride flux at benzodiazepine-sensitive GABAA receptors.
LGICGABAA receptorFlumazenilFlumazenil is a NAL with respect to GABA affinity and chloride flux at (most) GABAA receptor subtypes.
LGICGABAA receptorPentobarbitalPentobarbital is a PAM of GABA affinity and chloride flux and an allosteric agonist with respect to GABAA receptor gating.
LGICnAChRLidocaineLidocaine is a PAM of acetylcholine affinity but a NAM of acetylcholine-mediated cation flux at the nAChR.
LGICNMDA (GluN1/GluN2A)TCN-201TCN-201 is a NAM of glycine affinity and efficacy but a NAL of glutamate activity at the NMDA receptor.
VGICCaV1BayK8644BayK8644 is an allosteric agonist at CaV1 channels, a competitive antagonist of other dihydropyridines, a PAM with respect to diltiazem, and a NAM with respect to verapamil.
RTKFGFR1SSR128129ESSR128129E is NAL with respect to FGF2 affinity but a NAM of FGF2 efficacy to mediate phosphorylation of FRS2 and ERK1/2. It is a Type 3 tyrosine kinase inhibitor with respect to the ATP binding site.
  • BayK8644, methyl 2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl)phenyl]-1,4-dihydropyridine-3-carboxylate; ERK1/2, extracellular signal-regulated kinase 1/2; FGFR1, FGF receptor 1; FRS2, fibroblast growth factor receptor substrate 2; M-5MPEP, 2-[(3-methoxyphenyl)ethynyl]-5-methylpyridine; NAL, neutral allosteric ligand (see also Note 10).