Table 1.
Compound | DA Release | |||
---|---|---|---|---|
Head group | Linker | Inhibition (100 nM)a | IC50 (nM) and Imaxbb | |
bPiDDB 1 | bis-1,12-dodecane | NDc | 2.0±1.0d 63% |
|
bPiDB 8 | bis-1,10-decane | ND | 180±110 63% |
|
tPy3PiB 3 | tris-linker (unsaturated) | 40±12% | 0.2±0.07e 67% |
|
7 | bis-1,12-dodecane | 50±21% | 0.95±0.30 60% |
|
9 | bis-1,10-decane | 36±12% | 37.4±18.7 65% |
|
16 | tris-linker (unsaturated) | 83±2% | 3.22±1.36 67% |
|
bPyiQB 2 | rigid bis-linker | ND | 63±39f 59% |
|
12 | bis-1,12-dodecane | ND | 40±30 53% |
|
13 | bis-1,10-decane | ND | 70±50 95% |
|
18 | tris-linker (saturated) | 28±11% | ND | |
21 | tetrakis-linker | ND | 56±45 52% |
|
11 | rigid bis-linker | 18±18% | ND | |
14 | bis-1,12-dodecane | ND | 8.59±3.27 76% |
|
15 | bis-1,10-decane | ND | 9.91±9.23 74% |
|
19 | tris-linker (saturated) | 58±9% | 0.35±0.09 58% |
|
22 | tetrakis-linker | 84±4% | 205±132 64% |
|
tkP3HPPB 4 | tetrakis-linker | 41±15% | 3.0±3.0g 63% |
|
23 | tetrakis-linker | 40±23% | 30±16 64% |
Percentage inhibition at 100 nM is presented unless otherwise specified. Each value represents data from at least 3 independent experiments, each performed in duplicate.
IC50 and Imax from full concentration response assays; data from 4–6 independent experiments.
Not determined;
taken from results published in ref 15;
taken from results published in ref 13;
taken from results published in ref 12;
taken from results published in ref 14.