Table 11Structure Activity Relationship (SAR) Elucidation in A

EntryCIDSIDS/PR1R2/R3R4IC50 (μM)
Bcl-BBcl-XL
3ACID 1097158SID 124756734SCH2PhcyclohexylH4.15>20
4ACID 1048554SID 124756736SCH2Phdi-CH3H>20>20
5ACID 53301972SID 124756683SCH2-4-Cl-PhcyclohexylCH3>20>20
6ACID 53301955SID 124756686SCH2-4-Cl-PhcyclohexylF0.775>20
7ACID 53301988SID 124756687SCH2-4-Cl-PhcyclopentylH2.11>20
8A
ML258
CID 53301938SID 124756688SCH2-4-OCH3-PhcyclopentylH0.386>20
9ACID 53301978SID 124756684SCH2PhcyclohexylCH313.6>20
10ACID 53301942SID 124756691SCH2-4-F-PhcyclohexylCH38.14>20
11ACID 53301947SID 124756692SCH2PhcyclopentylOCH3>20>20
12ACID 53301949SID 124756689SCH2-4-F-PhcyclopentylH1.56>20
13ACID 53301939SID 124756721SCH2-4-OCH3-Phdi-CH3CH33.94>20
14ACID 53301968SID 124756722SCH2Phdi-CH3CH35.77>20
15ACID 53301957SID 124756723SCH2Phdi-CH3OCH34.03>20
16ACID 53301984SID 124756724SCH2-4-F-Phdi-CH3OCH3>20>20
17ACID 53301961SID 124756725SCH2-4-Cl-Phdi-CH3OCH3>20>20
18ACID 53301960SID 124756732SCH2PhcyclopentylF>20>20
19ACID 53301951124756695S2-methylallylcyclopentylH>20>20

From: Selective Bcl-2 Inhibitor Probes

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