Table 1 Relative efficacy (with respect to T3 response), rank, and EC50 (nM) and for compounds obtained for 3D myelin wrapping assay using AAs, 2D differentiation assay, and ELISA.

From: Artificial axons as a biomimetic 3D myelination platform for the discovery and validation of promyelinating compounds

Compound

Relative efficacy (relative to T3 response) and rank

EC50, nM

3D AAs

2D glass

3D AAs

2D glass

ELISA* (MBP expression)

Efficacy

Rank

Efficacy

Rank

Tasin-1 (B)

7.8 (0.5)

1

2.0 (0.2)

2

22

13

17

Tamoxifen (B)

6.4 (0.8)

2

2.0 (0.2)

2

8

2

88

Benztropine (A)

6.1 (0.6)

2

2.1 (0.1)

2

581

375

127

Clemastine (A)

4.3 (0.4)

3

1.4 (0.1)

Below T3 control

678

121

120

Amorolfine (B)

4.1 (0.4)

3

2.4 (0.2)

1

5

10

16

Ketoconazole (A)

3.0 (0.5)

4

1.6 (1.1)

3

507

315

470

Fasudil (A)

2.5 (0.3)

5

1.0 (0.1)

Below T3 control

–

339

260

Clobetasol (A)

2.4 (0.5)

5

1.6 (0.2)

3

1040

546

455

Quetiapine (A)

2.3 (0.4)

5

1.9 (0.2)

2

635

207

184

Miconazole (A)

1.9 (0.6)

6

1.5 (0.1)

3

623

397

302

Bazedoxifene (B)

1.8 (0.2)

6

0.6 (0.1)

Below T3 control

3

0.1

16

T3 (B)

1.0 (0.2)

7

1.0 (0.1)

5

16

7

96

  1. Uncertainty in relative efficacy is expressed parenthetically as standard error of the mean (SEM).
  2. Group (A)—compounds in this group had measured MBP-ELISA EC50 values within the range from 100 nM to 1 μM.
  3. Group (B)—compounds in this group had measured MBP-ELISA EC50 below 100 nM.
  4. *ELISA experiments were performed with a different batch of rOPCs than used in the 3D AA and 2D differentiation experiments.
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