Table 4: Potency and Efficacy for Compounds Identified in the LOPAC Library Screening.

Agonists Potency, µM (Re-Screen) Efficacy, % (Re-Screen)
retinoic acid 0.8 22.2
CGP-7930 2.7 (2.6) 18.2 (18.0)
CGP-13501 2.8 (2.3) 16.8 (15.0)
13-cis-retinoic acid 6.4 (2.9) 18.8 (15.5)
SKF-89145 hydrobromide 21.9 (20.6) 10.9 (16.5)
4-hydroxybenzhydrazide 24.6 (26.0) 11.5 (17.5)
Antagonists
Tranilast 0.7 (0.8) -86 (-81.8)
SB 205384 2.6 (2.5) -75 (-73.0)
NS-1619 5.2 (13.4) -58 (-75.7)
5-fluorouracil 5.2 (3.1) -72 (-71.1)

Potency (EC50 and IC50) values were calculated from full dose response curves in the absence and presence of T3 (1nM), respectively. Efficacy was defined as percentage of maximal induction (agonist mode) or inhibition (antagonist mode) relative to T3 set at 100% (100 nM for testing of agonist and 1 nM for antagonist activity). Average of re-screen values listed in parentheses.