Pharos : Ligand Details

Target Activities

Explore Associated and Predicted Targets

CACNA1G

Tclin

Voltage-dependent T-type calcium channel subunit alpha-1G

22 Activities

Items per page:

1 – 10 of 22

Activity Type	Activity Value -log(M)	Activity Reference	Publications (PubMed IDs)
IC50	7.19	J Med Chem, (2017) 60:23:9769	29116786

IC50	6.7	Bioorg. Med. Chem., (2011) 19:18:5628	21875808

IC50	6.25	Bioorg. Med. Chem. Lett., (2013) 23:24:6656	24220170

IC50	6.25	Bioorg. Med. Chem. Lett., (2014) 24:6:1565	24529871

IC50	6.08	Bioorg. Med. Chem. Lett., (2004) 14:13:3379	15177437

IC50	6.08	Bioorg. Med. Chem., (2007) 15:2:1091	17074493

IC50	6.08	Bioorg. Med. Chem. Lett., (2010) 20:14:4219	20621730

IC50	6.08	Bioorg. Med. Chem. Lett., (2013) 23:6:1887	23395659

IC50	6.07	Bioorg. Med. Chem. Lett., (2010) 20:14:4219	20621730

IC50	6	Bioorg. Med. Chem., (2010) 18:16:5938	20659804

KCNH2

Tclin

Potassium voltage-gated channel subfamily H member 2

19 Activities

Items per page:

1 – 10 of 19

Activity Type	Activity Value -log(M)	Activity Reference	Publications (PubMed IDs)
Ki	6.72	J. Med. Chem., (2007) 50:13:2931	17536794

Ki	6.45	J. Med. Chem., (2007) 50:13:2931	17536794

IC50	6.24	J Med Chem, (2017) 60:23:9769	29116786

IC50	6.09	J. Med. Chem., (2008) 51:20:6471	18817368

IC50	5.89	Bioorg. Med. Chem. Lett., (2015) 25:18:3941	26231163

IC50	5.87	Bioorg. Med. Chem. Lett., (2011) 21:19:5910	21843937

IC50	5.87	Bioorg Med Chem Lett, (2019) 29:10:1168	30928197

IC50	5.85	Bioorg. Med. Chem. Lett., (2004) 14:18:4771	15324906

IC50	5.85	Bioorg. Med. Chem. Lett., (2010) 20:9:2705	20382529

IC50	5.85	Bioorg. Med. Chem. Lett., (2011) 21:1:215	21126876

CACNA1H

Tclin

Voltage-dependent T-type calcium channel subunit alpha-1H

7 Activities

Items per page:

1 – 7 of 7

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	7.5		Bioorg. Med. Chem. Lett., (2010) 20:22:6375	20934333

IC50	6.89		Bioorg. Med. Chem. Lett., (2008) 18:2:474	18160281

IC50	6.89		J Med Chem, (2017) 60:23:9769	29116786

IC50	6.74		Bioorg. Med. Chem. Lett., (2015) 25:18:3941	26231163

IC50	6		Bioorg. Med. Chem., (2010) 18:16:5938	20659804

IC50	6		Bioorg. Med. Chem. Lett., (2013) 23:1:119	23200256

IC50	6.6	BLOCKER	http://www.ncbi.nlm.nih.gov/pubmed/18974361

CYP3A4

Tclin

Cytochrome P450 3A4

5 Activities

Items per page:

1 – 5 of 5

Activity Type	Activity Value -log(M)	Activity Reference	Publications (PubMed IDs)
IC50	6.89	J. Med. Chem., (2003) 46:9:1716	12699389

Ki	6.55	Drug Metab. Dispos., (2011) 39:7:1188	21447734

IC50	6.52	J. Med. Chem., (2012) 55:11:4896	22409598

AC50	6.5	None, None:None:None

IC50	6.33	Drug Metab. Dispos., (2013) 41:1:60	23033255

CACNA1I

Tclin

Voltage-dependent T-type calcium channel subunit alpha-1I

4 Activities

Items per page:

1 – 4 of 4

Activity Type	Activity Value -log(M)	Activity Reference	Publications (PubMed IDs)
IC50	5.8		10991994

IC50	6.9	J. Med. Chem., (2008) 51:20:6471	18817368

IC50	6.89	J Med Chem, (2017) 60:23:9769	29116786

IC50	6	Bioorg. Med. Chem., (2010) 18:16:5938	20659804

CACNA1C

Tclin

Voltage-dependent L-type calcium channel subunit alpha-1C

3 Activities

Items per page:

1 – 3 of 3

Activity Type	Activity Value -log(M)	Activity Reference	Publications (PubMed IDs)
	4.9		10991994

IC50	6.7	Bioorg. Med. Chem. Lett., (2015) 25:18:3941	26231163

IC50	6.6	J Med Chem, (2017) 60:23:9769	29116786

CYP2D6

Tclin

Cytochrome P450 2D6

3 Activities

Items per page:

1 – 3 of 3

Activity Type	Activity Value -log(M)	Activity Reference	Publications (PubMed IDs)
IC50	7.2	Bioorg. Med. Chem. Lett., (2013) 23:1:119	23200256

AC50	6.5	None, None:None:None

IC50	6.08	Drug Metab. Dispos., (2013) 41:1:60	23033255

CACNA1B

Tclin

Voltage-dependent N-type calcium channel subunit alpha-1B

2 Activities

Items per page:

1 – 2 of 2

Activity Type	Activity Value -log(M)	Activity Reference	Publications (PubMed IDs)
IC50	6.38	Bioorg. Med. Chem. Lett., (2010) 20:22:6375	20934333

IC50	5.87	Bioorg. Med. Chem. Lett., (2010) 20:9:2705	20382529

CACNA1A

Tchem

Voltage-dependent P/Q-type calcium channel subunit alpha-1A

1 Activities

Items per page:

1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
-	6.5			10665814

CACNA1E

Tchem

Voltage-dependent R-type calcium channel subunit alpha-1E

1 Activities

Items per page:

1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
-	6.4			10665814

SCN5A

Tclin

Sodium channel protein type 5 subunit alpha

1 Activities

Items per page:

1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.3		J Med Chem, (2017) 60:23:9769	29116786

SCN9A

Tclin

Sodium channel protein type 9 subunit alpha

1 Activities

Items per page:

1 – 1 of 1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)
IC50	6.3		J Med Chem, (2017) 60:23:9769	29116786