Compound Detail

CHEMBL328560

SULTHIAME

🧪 Phase III

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🧪 Phase III

NS(=O)(=O)c1ccc(N2CCCCS2(=O)=O)cc1

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL328560
Name	SULTHIAME
Phase	Phase III
Structure Type	MOL
InChI Key	HMHVCUVYZFYAJI-UHFFFAOYSA-N
Therapeutic	✓ Yes

Known Names

Conadil Ospolot RIKER 594 RIKER-594 Sulthiame Sultiame Sultiamo Trolone

Targets

108

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Mechanisms

Molecular Properties

290.4

MW (Da)

0.26

ALogP

HBA

HBD

97.5

PSA (Å²)

0.84

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
Chirality	Achiral

Flags

Natural Product

USAN Year

1962

Extended Properties

Molecular Formula	C10H14N2O4S2
MW	290.37
Aromatic Rings	1
Heavy Atoms	18
NP-Likeness	-2.28

Mechanism of Action

Mechanism	Action Type	Target	Direct	Efficacy
Carbonic anhydrase inhibitor	INHIBITOR	Carbonic anhydrase	✓	✓

Indications

Epilepsy Sleep Apnea, Obstructive

ATC Classification

N03AX03

sultiame

Level 1: NERVOUS SYSTEM

Level 2: ANTIEPILEPTICS

Activity Summary

Ki 108 meas. best 8.15

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Carbonic anhydrase 2 CHEMBL205	Ki	8.15	8.0534	7.0	29
Unchecked CHEMBL612545	Ki	8.11	6.3015	7.8	39
Carbonate dehydratase CHEMBL3745586	Ki	8.11	8.11	7.8	1
Carbonic anhydrase 9 CHEMBL3594	Ki	7.37	7.37	43.0	1
Alpha carbonic anhydrase CHEMBL1075028	Ki	7.34	7.34	45.2	2
Carbonic anhydrase 15 CHEMBL5973	Ki	7.19	7.19	65.0	1
Carbonic anhydrase CHEMBL1649055	Ki	6.91	6.91	123.0	1
Carbonic anhydrase 6 CHEMBL3025	Ki	6.87	6.87	134.0	1
Delta carbonic anhydrase CHEMBL3097982	Ki	6.77	6.77	169.0	1
AGAP002992-PA CHEMBL3399914	Ki	6.58	6.58	265.0	1
Astrosclerin-3 CHEMBL1944499	Ki	6.56	6.56	276.0	1
Carbonic anhydrase 1 CHEMBL261	Ki	6.43	6.43	374.0	25
Carbonic anhydrase, alpha family CHEMBL3621035	Ki	6.37	6.37	432.0	1
Carbonic anhydrase 2 CHEMBL6068	Ki	6.18	6.18	664.0	1
Carbonic anhydrase CHEMBL5931	Ki	5.99	5.99	1020.0	1
Carbonic anhydrase CHEMBL5337	Ki	5.97	5.97	1071.0	1
Beta-carbonic anhydrase 1 CHEMBL5631	Ki	5.29	5.29	5160.0	1

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Carbonic anhydrase 2	Ki	=	7.0	nM	8.15	Inhibition of recombinant human carbonic anhydrase 2 preincubated with enzyme fo...	33866238
Unchecked	Ki	=	7.8	nM	8.11	Inhibition of Sulfurihydrogenibium yellowstonense YO3AOP1 recombinant carbonic a...	22883029
Carbonate dehydratase	Ki	=	7.8	nM	8.11	Inhibition of recombinant Sulfurihydrogenibium yellowstonense YO3AOP1 carbonic a...	26691758
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrati...	19317447
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human cytosolic carbonic anhydrase 2 preincubated for 15 mins by s...	27485387
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human carbonic anhydrase-2 assessed as reduction in CO2 hydration ...	28511911
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human carbonic anhydrase 2 assessed as reduction in CO2 hydration ...	28025002
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human carbonic anhydrase 2 incubated for 15 mins by stopped-flow C...	26920803
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human carbonic anhydrase 2 preincubated for 15 mins by CO2 hydrase...	26832216
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human Carbonic anhydrase2 using CO2 as substrate preincubated for ...	26850377
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of recombinant human carbonic anhydrase-2 by stopped flow CO2 hydrase...	26691758
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human CA2 incubated for 15 mins prior to testing by stopped flow C...	26525863
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human recombinant carbonic anhydrase-2 by stopped flow CO2 hydrase...	26174556
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human carbonic anhydrase 2 pre-incubated for 15 mins by stopped-fl...	25882523
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrase...	25773015
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human recombinant carbonic anhydrase 2 by stopped-flow CO2 hydrati...	25533402
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human recombinant Carbonic anhydrase 2 compound preincubated for 1...	25129169
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human recombinant CA2 by stopped-flow CO2 assay	19520577
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of Helicobacter pylori beta-carbonic anhydrase by stopped-flow CO2 hy...	19450983
Carbonic anhydrase 2	Ki	=	9.0	nM	8.05	Inhibition of human recombinant carbonic anhydrase 2 by stopped flow CO2 hydrati...	19338333

Literature References

PubMed	DOI	Target Context	# Activities
26832216	10.1016/j.bmcl.2016.01.023	Unchecked	4
33866238	10.1016/j.ejmech.2021.113444	Unchecked	4
25773015	10.1016/j.bmc.2015.02.045	Unchecked	3
37468498	10.1038/s41467-023-40064-9	Histamine H1 receptor	3
24792813	10.1016/j.bmc.2014.04.006	Unchecked	3
37468498	10.1038/s41467-023-40064-9	Nuclear receptor subfamily 1 group I member 2	3
34731762	10.1016/j.ejmech.2021.113956	Unchecked	3
25129169	10.1016/j.bmc.2014.07.048	Unchecked	3
26174556	10.1016/j.bmcl.2015.06.079	Unchecked	3
-	10.6019/CHEMBL4495565	SARS-CoV-2	2
19846301	10.1016/j.bmcl.2009.10.009	Carbonic anhydrase 2	2
21757360	10.1016/j.bmc.2011.06.038	Unchecked	2
26525863	10.1016/j.bmcl.2015.10.074	Unchecked	2
26850377	10.1016/j.bmc.2016.01.037	Unchecked	2
22883029	10.1016/j.bmc.2012.07.024	Unchecked	2
28511911	10.1016/j.bmc.2017.05.007	Unchecked	2
24316122	10.1016/j.bmcl.2013.11.030	Unchecked	2
24314394	10.1016/j.bmcl.2013.11.021	Unchecked	2
28025002	10.1016/j.bmcl.2016.12.035	Unchecked	2
-	10.6019/CHEMBL4651402	SARS-CoV-2	2

Data from ChEMBL 36 via Core Engine