Uncoupling Neuroprotection from Immunosuppression: the Discovery of ILS-920 - Accounts in Drug Discovery Case Studies in Medicinal Chemistry - page 323

Table 14.1 Biological activities and kinetic constants of immunophilin ligands.

Cortical neuron
survival
(EC 50 , mM)

[ 3 H]-DA uptake
(EC 50 , mM)

T-cell inhibition
(IC 50 , mM)

Neurite outgrowth
(EC 50 , mM)

FKBP12 binding
(K d , nM) Compounds

FK506 0.001 0.45 0.01 0.049 0.33 0.03

(lit. 0.4)

NT a

ILS-920 45 0.54 0.15 110 11

WYE-592 0.15 0.42 0.7 NT 4.7 0.4

Rapamycin 0.005 1.6 1.3 410 0.33 0.03

3-Normeridamycin 410 200 8.8 0.11 50

a NT ¼ not tested.