You are tasked with identifying lead molecules for a protein tyrosine kinase cal

Question

You are tasked with identifying lead molecules for a protein tyrosine kinase called PTKA1. All lead molecules must be highly specific for inhibition of PTKA1 over its isoform PTKA2. More specifically, any lead molecule must have at least a low nano-molar IC50 against PTKA1 and be 10x more potent an inhibitor of PTKA1 than PTKA2. After running a PTKA1 screen and PTKA2 counter-screen, you obtain the following results. Circle all potential lead molecules.

Molecule

IC50 (PTKA1)

IC50 (PTKA2)

1

40 pM

20 M

2

1 pM

5 pM

3

7 nM

5 pM

4

4 nM

50 nM

5

100 nM

100 M

Molecule

IC50 (PTKA1)

IC50 (PTKA2)

1

40 pM

20 M

2

1 pM

5 pM

3

7 nM

5 pM

4

4 nM

50 nM

5

100 nM

100 M

Explanation / Answer

Molecule 1 is more than 10x more potent inhibitor of PTKA1 than PTKA2 as for PTKA1 it is required in pM and and for PTKA 2 it is required in micromolar.

Molecules 5 is also a potential lead molecule as it is required nano molar for PTKA 1 and for PTKA2 it is required in micromolar.

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