IC50 (binding)
|
= 3050 nM
|
BindingDB_Patents: Inhibition Assay. The inhibition of human CYP2A6-mediated 7-hydroxy coumarin formation was evaluated in the presence of 95 selected test compounds in a standard assay (Greenlee et al., J Pharmacol Exp Ther, 1978). Our first studies were with highly purified human CYP2A6 that provided a convenient and relatively high-throughput measure of CYP2A6 inhibition.
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
= 3050 nM
|
BindingDB_Patents: Inhibition Assay. The inhibition of human CYP2A6-mediated 7-hydroxy coumarin formation was evaluated in the presence of 95 selected test compounds in a standard assay (Greenlee et al., J Pharmacol Exp Ther, 1978). Our first studies were with highly purified human CYP2A6 that provided a convenient and relatively high-throughput measure of CYP2A6 inhibition.
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
= 7800 nM
|
BindingDB_Patents: Inhibition Assay. The inhibition of human CYP2A6-mediated 7-hydroxy coumarin formation was evaluated in the presence of 95 selected test compounds in a standard assay (Greenlee et al., J Pharmacol Exp Ther, 1978). Our first studies were with highly purified human CYP2A6 that provided a convenient and relatively high-throughput measure of CYP2A6 inhibition.
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
= 7800 nM
|
BindingDB_Patents: Inhibition Assay. The inhibition of human CYP2A6-mediated 7-hydroxy coumarin formation was evaluated in the presence of 95 selected test compounds in a standard assay (Greenlee et al., J Pharmacol Exp Ther, 1978). Our first studies were with highly purified human CYP2A6 that provided a convenient and relatively high-throughput measure of CYP2A6 inhibition.
|
ChEMBL.
|
No reference
|
IC50 (binding)
|
= 7800 nM
|
BindingDB_Patents: Inhibition Assay. The inhibition of human CYP2A6-mediated 7-hydroxy coumarin formation was evaluated in the presence of 95 selected test compounds in a standard assay (Greenlee et al., J Pharmacol Exp Ther, 1978). Our first studies were with highly purified human CYP2A6 that provided a convenient and relatively high-throughput measure of CYP2A6 inhibition.
|
ChEMBL.
|
No reference
|
IC50 (ADMET)
|
= 4.1 uM
|
Inhibitory concentration value against human cytochrome P-450 2E1
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
= 4.1 uM
|
Inhibitory concentration value against human cytochrome P-450 2E1
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
= 7.8 uM
|
Inhibitory concentration value against human cytochrome P-450 2A6
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
= 7.8 uM
|
Inhibitory concentration value against human cytochrome P-450 2A6
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
= 57 uM
|
Inhibitory concentration value against human cytochrome P-450 3A4
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
= 57 uM
|
Inhibitory concentration value against human cytochrome P-450 3A4
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
= 70.8 uM
|
Inhibitory concentration value against human cytochrome P-450 2B6
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
= 70.8 uM
|
Inhibitory concentration value against human cytochrome P-450 2B6
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
= 99.2 uM
|
Inhibitory concentration against human cytochrome P-450 2C9
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
= 99.2 uM
|
Inhibitory concentration against human cytochrome P-450 2C9
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
= 178 uM
|
Inhibitory concentration value against human cytochrome P-450 2C19
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
= 178 uM
|
Inhibitory concentration value against human cytochrome P-450 2C19
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
> 400 uM
|
Inhibitory concentration value against human cytochrome P-450 2D6
|
ChEMBL.
|
15634016
|
IC50 (ADMET)
|
> 400 uM
|
Inhibitory concentration value against human cytochrome P-450 2D6
|
ChEMBL.
|
15634016
|
Ki (ADMET)
|
= 1.2 uM
|
Effect on coumarin 7-hydroxylation by human Cytochrome P-450 2A6
|
ChEMBL.
|
15634016
|
Ki (ADMET)
|
= 1.2 uM
|
Effect on coumarin 7-hydroxylation by human Cytochrome P-450 2A6
|
ChEMBL.
|
15634016
|
Ratio (ADMET)
|
= 0.53
|
Ratio of inhibition of human cytochrome P-450 2E1 to 2A6 was determined; Expressed as IC50(CYP2E1)/IC50(CYP2A6)
|
ChEMBL.
|
15634016
|
Ratio (ADMET)
|
= 7.3
|
Ratio of inhibition of human cytochrome P-450 3A4 to 2A6 was determined; Expressed as IC50(CYP3A4)/IC50(CYP2A6)
|
ChEMBL.
|
15634016
|
Ratio (ADMET)
|
= 9.1
|
Ratio of inhibition of human cytochrome P-450 2B6 to 2A6 was determined; Expressed as IC50(CYP2B6)/IC50(CYP2A6)
|
ChEMBL.
|
15634016
|
Ratio (ADMET)
|
= 13
|
Ratio of inhibition of human cytochrome P-450 2C9 to 2A6 was determined; Expressed as IC50(CYP2C9)/IC50(CYP2A6)
|
ChEMBL.
|
15634016
|
Ratio (ADMET)
|
= 23
|
Ratio of inhibition of human cytochrome P-450 2C19 to 2A6 was determined; Expressed as IC50(CYP2C19)/IC50(CYP2A6)
|
ChEMBL.
|
15634016
|
Ratio (ADMET)
|
> 51
|
Ratio of inhibition of human cytochrome P-450 2D6 to 2A6 was determined; Expressed as IC50(CYP2D6)/IC50(CYP2A6)
|
ChEMBL.
|
15634016
|