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| # | Molecule ChEMBL ID | Compound Key | Standard Type | Standard Relation | Standard Value | Standard Text Value | Standard Units | pChEMBL Value | Comment | Assay ChEMBL ID | Assay Description | BAO Label | Assay Organism | Target ChEMBL ID | Target Name | Target Organism | Target Type | Document ChEMBL ID | Source Description | Cell ChEMBL ID | |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 1. |
AZT-MP
|
Ratio
|
=
|
1.08
|
---
|
---
|
---
|
---
|
Ratio of Kcat to Km for HIV1 reverse transcriptase M41L/D67N/L210W/T215Y mutant assessed as nucleotide excision activity in presence of 10 uM dCTP
|
assay format
|
Human immunodeficiency virus 1
|
Human immunodeficiency virus type 1 reverse transcriptase
|
Human immunodeficiency virus 1
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 2. |
AZT-MP
|
Ratio
|
=
|
6.8
|
---
|
---
|
---
|
---
|
Ratio of Kcat/Km for HIV1 reverse transcriptase M41L/D67N/L210W/T215Y mutant to Kcat/Km for wild-type reverse transcriptase assessed as nucleotide excision activity in presence of 0.5 uM dCTP
|
assay format
|
Human immunodeficiency virus 1
|
Unchecked
|
---
|
UNCHECKED
|
Scientific Literature
| ||||||
| 3. |
AZTMP
|
IC50
|
=
|
5000.0
|
---
|
nM
|
5.30
|
---
|
Inhibitory concentration at which there is accumulation of UDP-[3H]-GlcNAc in the lumen of the Golgi membranes.
|
cell membrane format
|
Oryctolagus cuniculus
|
Unchecked
|
---
|
UNCHECKED
|
Scientific Literature
| ||||||
| 4. |
AZTMP
|
T1/2
|
=
|
4.0
|
---
|
hr
|
---
|
---
|
Half life evaluated in Total Cell Extract(TCE).
|
assay format
|
---
|
ADMET
|
---
|
ADMET
|
Scientific Literature
| ||||||
| 5. |
Azidothymidine monophosphate
|
Activity
|
---
|
---
|
---
|
---
|
---
|
substrate [+]
|
TP_TRANSPORTER: efflux in CEM-r1 cells
|
cell-based format
|
---
|
Multidrug resistance-associated protein 4
|
Homo sapiens
|
SINGLE PROTEIN
|
TP-search Transporter Database
| ||||||
| 6. |
AZT-MP
|
Activity
|
---
|
---
|
---
|
---
|
---
|
Active
|
Binding affinity to 200 nM wild type HIV1 LAI reverse transcriptase assessed as ATP-mediated excision of zidovudine-monophosphate from chain terminated DNA/DNA template/primer duplex at 100 uM
|
single protein format
|
Human immunodeficiency virus 1
|
Human immunodeficiency virus type 1 reverse transcriptase
|
Human immunodeficiency virus 1
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 7. |
AZT-MP
|
Activity
|
---
|
---
|
---
|
---
|
---
|
Active
|
Binding affinity to 200 nM HIV1 LAI reverse transcriptase M41L/L210W/T215Y mutant assessed as ATP-mediated excision of zidovudine-monophosphate from chain terminated DNA/DNA template/primer duplex at 100 uM
|
assay format
|
Human immunodeficiency virus 1
|
Human immunodeficiency virus type 1 reverse transcriptase
|
Human immunodeficiency virus 1
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 8. |
AZTMP
|
Kcat/Km
|
=
|
1000.0
|
---
|
/M/s
|
---
|
---
|
Ratio of kcat/km for human recombinant TMPK by Michaelis-Menten equation analysis
|
single protein format
|
Homo sapiens
|
Thymidylate kinase
|
Homo sapiens
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 9. |
AZT-MP
|
Ratio
|
=
|
1.3
|
---
|
---
|
---
|
---
|
Ratio of Kcat to Km for HIV1 reverse transcriptase M41L/D67N/L210W/T215Y mutant assessed as nucleotide excision activity in presence of 0.5 uM dCTP
|
assay format
|
Human immunodeficiency virus 1
|
Human immunodeficiency virus type 1 reverse transcriptase
|
Human immunodeficiency virus 1
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 10. |
AZT-MP
|
Km
|
=
|
1400000.0
|
---
|
nM
|
---
|
---
|
Activity of HIV1 reverse transcriptase M41L/D67N/L210W/T215Y mutant assessed as nucleotide excision activity in presence of 0.5 uM dCTP
|
assay format
|
Human immunodeficiency virus 1
|
Human immunodeficiency virus type 1 reverse transcriptase
|
Human immunodeficiency virus 1
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 11. |
AZTMP
|
Km
|
=
|
7600.0
|
---
|
nM
|
---
|
---
|
Activity for human recombinant TMP kinase
|
single protein format
|
Homo sapiens
|
Thymidylate kinase
|
Homo sapiens
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 12. |
AZTMP
|
Kcat
|
=
|
0.018
|
---
|
/s
|
---
|
---
|
Activity for human recombinant TMP kinase
|
single protein format
|
Homo sapiens
|
Thymidylate kinase
|
Homo sapiens
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 13. |
AZTMP
|
Ki
|
=
|
10000.0
|
---
|
nM
|
5.00
|
---
|
In Vitro inhibition of Thymidine Monophosphatase Kinase of Mycobacterium tuberculosis (TMPKm)
|
single protein format
|
Mycobacterium tuberculosis
|
Thymidylate kinase
|
Mycobacterium tuberculosis
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 14. |
AZT-MP
|
Activity
|
---
|
---
|
---
|
---
|
---
|
Active
|
Binding affinity to HIV1 LAI reverse transcriptase M41L/L210W/T215Y/M184V mutant assessed as ATP-mediated excision of zidovudine-monophosphate from chain terminated RNA/DNA template/primer duplex
|
assay format
|
Human immunodeficiency virus 1
|
Human immunodeficiency virus type 1 reverse transcriptase
|
Human immunodeficiency virus 1
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 15. |
AZT-MP
|
Ratio
|
=
|
1.1
|
---
|
---
|
---
|
---
|
Selectivity ratio of Kd for excision of zidovudine-monophosphate from chain terminated DNA/DNA template/primer duplex in HIV1 LAI reverse transcriptase M41L/L210W/T215Y/K65R/G333D mutant to Kd for excision of zidovudine-monophosphate from chain terminated DNA/DNA template/primer duplex in wild type HIV1 LAI reverse transcriptase by gel shift mobility assay
|
assay format
|
Human immunodeficiency virus 1
|
Unchecked
|
---
|
UNCHECKED
|
Scientific Literature
| ||||||
| 16. |
AZT-MP
|
Ratio
|
=
|
0.19
|
---
|
---
|
---
|
---
|
Ratio of Kcat to Km for HIV1 reverse transcriptase assessed as nucleotide excision activity in presence of 0.5 uM dCTP
|
single protein format
|
Human immunodeficiency virus 1
|
Human immunodeficiency virus type 1 reverse transcriptase
|
Human immunodeficiency virus 1
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 17. |
AZT-MP
|
Ratio
|
=
|
1.2
|
---
|
---
|
---
|
---
|
Ratio of Kcat/Km for HIV1 reverse transcriptase in presence of 0.5 uM dCTP to Kcat/Km for reverse transcriptase in presence of 10 uM dCTP by nucleotide excision activity assay
|
single protein format
|
Human immunodeficiency virus 1
|
Human immunodeficiency virus type 1 reverse transcriptase
|
Human immunodeficiency virus 1
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 18. |
AZT 5`-phosphate
|
Internalisation
|
=
|
0.06
|
---
|
%
|
---
|
---
|
In Vitro detection by Gray and Whittaker method for % of internalization by comparing with external nucleoside of 2000 nM/g
|
organism-based format
|
Mus musculus
|
Mus musculus
|
Mus musculus
|
ORGANISM
|
Scientific Literature
| ||||||
| 19. |
AZTMP
|
Ki
|
=
|
10000.0
|
---
|
nM
|
5.00
|
---
|
Inhibitory activity against thymidine monophosphate kinase (TMPK) in Mycobacterium tuberculosis
|
single protein format
|
Mycobacterium tuberculosis
|
Thymidylate kinase
|
Mycobacterium tuberculosis
|
SINGLE PROTEIN
|
Scientific Literature
| ||||||
| 20. |
AZTMP
|
IC50
|
=
|
5000.0
|
---
|
nM
|
5.30
|
---
|
The compound was tested for extent of UDP-[3H]-GlcNAc accumulation into the lumen of the Golgi membranes.
|
assay format
|
Oryctolagus cuniculus
|
Unchecked
|
---
|
UNCHECKED
|
Scientific Literature
|
Showing 1-20
out of 80 records
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