Chemistry Reference
In-Depth Information
N
N
HO
2
C
O
N
N
O
(a)
O
O
N
O
H
N
Cl
N
NH
2
NH
+
A
Cl
Cl
N
NH
2
NH
H
Cl
N
H
CO
2
H
O
IL-2
O
M
Parent compound
IC
50
: 3
Multiple carboxylic
acid containing hits
M
Advanced compound
IC
50
: 0.060
µ
µ
CO
2
H
OH
OO
CO
2
H
(b)
O
CO
2
H
OO
O
H
N
N
S
OO
N
O
N
H
S
H
N
Caspase
S
S
S
H
H
OH
S
N
H
OH
Caspase-3
N
H
O
O
HO
2
C
O
HO
2
C
HO
2
C
M
Linked compound
K
i
: 2.8
µ
M
Advanced compound
K
i
: 0.02
µ
Extender
Hit
N(CH
2
COO
-
)
2
Cu
2+
(c)
O
O
O
H
2
N
N
S
Human carbonic
anhydrase II
N(CH
2
COO
-
)
2
Cu
2+
O
N
H
O
O
O
H
2
N
O
S
K
i
: 1.5
µ
M
Parent compound
K
i
: 0.011
µ
M
Advanced compound
Figure 10.3
Examples of starting points and progressed compounds using various capture methods.
