Table 1 Binding and competition potencies in RBA.

From: Pharmacological characterization of mutant huntingtin aggregate-directed PET imaging tracer candidates

Compound ID

Kd (nM)

IC50 (nM)

Exon1-Q46

Q46

Exon1-Q46

Q46

1 (CHDI-180)

2.6 ± 0.9

7.7 ± 3.3

1.3 ± 0.7

1.2 ± 0.5

2 (CHDI-626)

4.5 ± 0.8

5.8 ± 1.7

2.9 ± 0.6

3.6 ± 1.6

3

2.5 ± 0.6

4.7 ± 0.2

1.2 ± 0.4

1.8 ± 0.8

4

5.5 ± 1.3

7.8 ± 4.1

0.4 ± 0.1

0.7 ± 0.1

5

5.2 ± 1.8

8.7 ± 4.0

5.8 ± 1.7

4.7 ± 2.4

6 (PiB)

(–)a

(–)a

72.5 ± 0.4

 > 333

7 (T808)

(–)a

(–)a

 > 333

 > 333

8

n.a

139.5 ± 36.9*

9.9 ± 1.0

10.3 ± 2.7

  1. Mean values and standard deviations; see structures of compounds in Supplementary Fig. S1. *Higher protein concentrations (10–30 µM) were applied. aNot determinable because TB ≅ NSB.
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