Data


The tested compounds are listed bellow with the determined Michaelis constant Km, inhibition constant Ki and inhibition type.

 

Compounds

Km

[µM]

Ki

[µM]

Type of inhibition and

Remarks

1

70

1.4

Uncompetitive

2

62

319

Uncompetitive

3

44

14.5

Uncompetitive

4

61

16.4

Competitive

5

61

337

Uncompetitive

6

61

28'000

Competitive

7

60

44'000

Mixed

8

60

 5'520

Uncompetitive

9

54

328

Uncompetitive

10

43

15'000

Competitive

11

76

3'680

Uncompetitive

12

39

39'500

Competitive

13

45

X

No inhibitor

14

45

24'900

Uncompetitive

15

--

--

Hydrolyses in the testing conditions!

Ki value larger than compound 2

16

--

--

Hydrolyses in the testing conditions!

Ki value larger than compound 2

17

--

--

Slow-binding

18

--

--

Formation of pyrrole with 5-aminlevulinic acid. Not possible to test!

19

--

--

UV absorption in the range used for the pyrrole formation determination

20

--

--

UV absorption in the range used for the pyrrole formation determination

All the compounds are drawn in their diketo form. In solution they are present as a mixture of the keto and the enol form. The following table gives the percentage of the enol form present in CDCl3 as determined by 1H-NMR. The determinations of the enol content were performed using concentrations comprised between 5 and 20 mM.

compounds

1

2

3

4

5

8

9

10

11

Enol %

90

71

81

97

90

61

98

41

85


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