Table 7Structure-Activity relationship study*

Image ml109fu11.jpg
NoSIDCIDR1R2R3R4R5R6XYEC50Emax
126755506661788HH
Image ml109fu12.jpg
OMeHNHAcNHO1.16101
22921639316759579HHBnOMeHNHAcNHO0.2999.8
32921699817757110HHn-BuOMeHNHAcNHO0.83112
42921813417757294HH
Image ml109fu13.jpg
OMeHNHAcNHO3.9870.3
52921699717757109HHHOMeHNHAcNHOn.d.39.5
62921815417757314HHBnOMeHNHAcNO0.9697.4
75765504625246367HOMeBnOMeHNHAcNHO4.4849.1
82675550625246343HOHBnOMeHNHAcNHO0.09100
92921813517757295HH
Image ml109fu14.jpg
OMeHNHAcNHOn.d.10.1
102921699917757111HH
Image ml109fu15.jpg
OMeHNHAcNHOn.d.19.7
112921813617757296HH
Image ml109fu16.jpg
OMeHNHAcNHO0.43102.5
1210307333149789101OHHBnOMeHNHAcNHO0.3393.3
1310307333249789102HHBnHHNHAcNHO1.8636.8
1410307333349789103HFBnOMeHNHAcNHO0.2894.7
15292169692887852HH
Image ml109fu17.jpg
OMeHNHAcNHO5.0975.1
162921814117757301HHBnOMeHOMeNHO2.1646.3
1710307333749789106HHBnOMeHHNHO2.5725.6
1810307333849789107HHBnOMeNHAcHNHO4.3424.8
1910307333946190126HHBnOMeHNHAcNHS0.0895.7
202921698917757102HH
Image ml109fu18.jpg
OMeHNHAcNO0.9359
2110307334049789108HOHBnOMe__NH_n.d.17.7
2210307334149789109HNH2BnOMeHNHAcNHO3.7872.6
2310307334249789110HNHMsBnOMeHNHAcNHO0.9890.8
242921814017757300HHBnOMeHCNNHOn.d.11.7
2510307334349789111HHBnOMeFHNHOn.d.7.4
2610307334449789112HOHBnOMeHNHAcNHS0.01869.6
2710307334549789113HOHBnOMeHNHAcNO0.5598.6
*

All analogs were synthesized. Activities (EC50) in μM were obtained from the Elisa assay (AID-2104). Emax is expressed as % of the maximal response of CID-25246343/ML109, set at 100%.

From: Identification of Potent and Selective Thyroid Stimulating Hormone Receptor Agonists

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