ketoconazole
Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients.
Ligand Summary
PubChem: 3823
Guide to Pharmacology: 2568
ChEMBL: CHEMBL157101
DrugCentral: 1527
LyCHI: P3TD9W5HJJWL
Target Activities
CYP3A4
Cytochrome P450 3A4
75 Activities
Items per page:
1 – 10 of 75
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
Ki | 7 | |||||
IC50 | 9 | J. Med. Chem., (2016) 59:7:3340 | ||||
IC50 | 8.4 | Bioorg. Med. Chem. Lett., (2009) 19:18:5376 | ||||
IC50 | 8.4 | J. Med. Chem., (2016) 59:7:3340 | ||||
Ki | 8.15 | Drug Metab. Dispos., (2013) 41:4:814 | ||||
IC50 | 8.13 | J Med Chem, (2016) 59:18:8535 | ||||
IC50 | 8.11 | J. Nat. Prod., (2011) 74:1:102 | ||||
IC50 | 8.04 | J Med Chem, (2016) 59:18:8535 | ||||
IC50 | 8.01 | Drug Metab. Dispos., (2013) 41:4:814 | ||||
IC50 | 7.96 | J. Med. Chem., (2010) 53:10:3887 | ||||
CYP17A1
Steroid 17-alpha-hydroxylase/17,20 lyase
23 Activities
Items per page:
1 – 10 of 23
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 7.58 | J. Med. Chem., (1995) 38:13:2463 | ||||
IC50 | 7.58 | J. Med. Chem., (1995) 38:21:4191 | ||||
IC50 | 7.58 | J. Med. Chem., (1996) 39:17:3319 | ||||
Ki | 7.42 | J. Med. Chem., (1998) 41:6:902 | ||||
Ki | 7.42 | J. Med. Chem., (2015) 58:5:2077 | ||||
IC50 | 7.32 | Bioorg Med Chem Lett, (2016) 26:23:5825 | ||||
IC50 | 7.19 | J. Med. Chem., (1996) 39:17:3319 | ||||
IC50 | 7.19 | J. Med. Chem., (1995) 38:13:2463 | ||||
IC50 | 7.19 | J. Med. Chem., (1995) 38:21:4191 | ||||
IC50 | 7.14 | J. Med. Chem., (2008) 51:16:5009 | ||||
CYP11B1
Cytochrome P450 11B1, mitochondrial
12 Activities
Items per page:
1 – 10 of 12
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 6.94 | Bioorg Med Chem Lett, (2016) 26:23:5825 | ||||
IC50 | 6.9 | J. Med. Chem., (2008) 51:16:5009 | ||||
IC50 | 6.9 | J. Med. Chem., (2010) 53:13:5049 | ||||
IC50 | 6.9 | ACS Med. Chem. Lett., (2011) 2:1:2 | ||||
IC50 | 6.9 | ACS Med. Chem. Lett., (2011) 2:8:559 | ||||
IC50 | 6.9 | None, (2016) None:None:None | ||||
IC50 | 6.65 | J. Med. Chem., (2005) 48:5:1563 | ||||
IC50 | 6.65 | J. Med. Chem., (2005) 48:21:6632 | ||||
IC50 | 6.65 | J. Med. Chem., (2006) 49:7:2222 | ||||
IC50 | 6.65 | None, (2016) None:None:None | ||||
CYP11B2
Cytochrome P450 11B2, mitochondrial
12 Activities
Items per page:
1 – 10 of 12
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 7.17 | J. Med. Chem., (2008) 51:16:5009 | ||||
IC50 | 7.17 | J. Med. Chem., (2010) 53:13:5049 | ||||
IC50 | 7.17 | ACS Med. Chem. Lett., (2011) 2:1:2 | ||||
IC50 | 7.17 | ACS Med. Chem. Lett., (2011) 2:8:559 | ||||
IC50 | 7.17 | None, (2016) None:None:None | ||||
IC50 | 7.09 | J. Med. Chem., (2005) 48:5:1563 | ||||
IC50 | 7.09 | J. Med. Chem., (2005) 48:21:6632 | ||||
IC50 | 7.09 | J. Med. Chem., (2006) 49:7:2222 | ||||
IC50 | 7.09 | None, (2016) None:None:None | ||||
IC50 | 7.09 | None, (2016) None:None:None | ||||
CYP24A1
1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial
11 Activities
Items per page:
1 – 10 of 11
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
Ki | 7.48 | J. Med. Chem., (2014) 57:18:7702 | ||||
Ki | 7.46 | Eur. J. Med. Chem., (2014) 87:None:39 | ||||
IC50 | 6.9 | Bioorg. Med. Chem., (2010) 18:14:4939 | ||||
IC50 | 6.51 | J. Med. Chem., (2004) 47:27:6854 | ||||
IC50 | 6.51 | Bioorg. Med. Chem., (2010) 18:14:4939 | ||||
IC50 | 6.33 | Eur. J. Med. Chem., (2014) 87:None:39 | ||||
IC50 | 6.33 | J. Med. Chem., (2014) 57:18:7702 | ||||
IC50 | 6.3 | Bioorg Med Chem, (2017) 25:20:5629 | ||||
IC50 | 6.3 | Bioorg Med Chem, (2017) 25:15:4076 | ||||
IC50 | 6.28 | Bioorg. Med. Chem., (2010) 18:14:4939 | ||||
KCNH2
Potassium voltage-gated channel subfamily H member 2
6 Activities
Items per page:
1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 5.72 | Bioorg. Med. Chem. Lett., (2003) 13:16:2773 | ||||
IC50 | 5.72 | Bioorg. Med. Chem. Lett., (2005) 15:11:2886 | ||||
IC50 | 5.72 | J. Med. Chem., (2009) 52:14:4266 | ||||
IC50 | 5.72 | J. Med. Chem., (2009) 52:14:4266 | ||||
IC50 | 5.72 | Bioorg. Med. Chem., (2008) 16:11:6252 | ||||
IC50 | 5.72 | Eur. J. Med. Chem., (2011) 46:2:618 | ||||
CYP19A1
Aromatase
6 Activities
Items per page:
1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 7.4 | J. Med. Chem., (2006) 49:7:2222 | ||||
IC50 | 7.22 | Bioorg. Med. Chem. Lett., (2010) 20:10:3050 | ||||
Ki | 6.4 | Bioorg. Med. Chem. Lett., (2012) 22:1:718 | ||||
Ki | 6.4 | Bioorg. Med. Chem. Lett., (2012) 22:1:718 | ||||
IC50 | 6.1 | J. Nat. Prod., (2008) 71:11:1793 | ||||
IC50 | 6.05 | J. Nat. Prod., (2007) 70:3:353 | ||||
CYP51A1
Lanosterol 14-alpha demethylase
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
Ki | 7.61 | J. Med. Chem., (1993) 36:15:2235 | ||||
Ki | 7.2 | J. Med. Chem., (1993) 36:15:2235 | ||||
Kd | 6.96 | Bioorg. Med. Chem., (2008) 16:1:209 | ||||
Kd | 6.96 | Antimicrob. Agents Chemother., (2009) 53:3:1157 | ||||
IC50 | 6.72 | Drug Metab. Dispos., (2007) 35:3:493 | ||||
SLC6A4
Sodium-dependent serotonin transporter
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
Ki | 6.55 | None, None:None:None | ||||
IC50 | 6.28 | None, None:None:None | ||||
CYP3A5
Cytochrome P450 3A5
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 6.92 | None, (2015) None:None:None | ||||
IC50 | 6.92 | None, (2015) None:None:None | ||||
CYP27B1
25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 6.47 | Bioorg Med Chem, (2017) 25:20:5629 | ||||
IC50 | 6.47 | |||||
KCNA10
Potassium voltage-gated channel subfamily A member 10
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
6.3 | ||||||
HSP90AA1
Heat shock protein HSP 90-alpha
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
AC50 | 6.36 | None, None:None:None | ||||
CYP4F2
Phylloquinone omega-hydroxylase CYP4F2
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
Ki | 6.13 | Drug Metab. Dispos., (2011) 39:2:191 | ||||
ABCB1
Multidrug resistance protein 1
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
---|---|---|---|---|---|---|
IC50 | 6 | J. Med. Chem., (2003) 46:9:1716 | ||||