Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T54644 | Target Info | |||
| Target Name | Voltage-gated calcium channel alpha Cav3.2 (CACNA1H) | ||||
| Synonyms |
Voltage-gated calcium channel subunit alpha Cav3.2; Voltage-dependent T-type calcium channel subunit alpha-1H; Low-voltage-activated calcium channel alpha1 3.2 subunit
Click to Show/Hide
|
||||
| Target Type | Successful Target | ||||
| Gene Name | CACNA1H | ||||
| Biochemical Class | Voltage-gated ion channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 13 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4226674
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461292
Click to Show/Hide
|
||||
| Activity |
IC50 = 54000 nM
|
[1] | |||
| Compound Name |
Chembl4227450
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461276
Click to Show/Hide
|
||||
| Activity |
IC50 = 64000 nM
|
[1] | |||
| Compound Name |
Chembl4225603
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461282
Click to Show/Hide
|
||||
| Activity |
IC50 = 95000 nM
|
[1] | |||
| Compound Name |
6H-Pyrimido[5,4-b][1,4]oxazin-7(8H)-one, 2-[[[trans-4-[(1R)-1-amino-2-(7-fluoro-2-oxo-1(2H)-quinoxalinyl)ethyl]cyclohexyl]amino]methyl]-
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3355573; SCHEMBL1375934; SCHEMBL1375938; BDBM50023589; SB19220
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[2] | |||
| Compound Name |
Auglurant
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
VU0424238; N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide; CHEMBL2386850; UNII-GRN8X62ZW2; GRN8X62ZW2; SCHEMBL12499337; VU238; EX-A2936; BDBM50257064; MFCD28386341; VU 238; 2-PyridinecarboxaMide, N-(5-fluoro-2-pyridinyl)-6-Methyl-4-(5-pyriMidinyloxy)-; HY-16617; CS-0009173; VU 0424238; YU-0424238; J3.655.475D; 2-PyridinecarboxaMide,N-(5-fluoro-2-pyridinyl)-6-Methyl-4-(5-pyriMidinyloxy)-; N-(5-Fluoro-2-pyridinyl)-6-methyl-4-(5-pyrimidinyloxy)-2-pyridinecarboxamide; N-(5-fluoropyridin-2-yl)-6-methyl-4-pyrimidin-5-yloxypyridine-2-carboxamide
Click to Show/Hide
|
||||
| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Chembl4229218
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461290
Click to Show/Hide
|
||||
| Activity |
IC50 = 109000 nM
|
[1] | |||
| Compound Name |
Chembl4227653
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461296
Click to Show/Hide
|
||||
| Activity |
IC50 = 110000 nM
|
[1] | |||
| Compound Name |
Chembl4227740
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461278
Click to Show/Hide
|
||||
| Activity |
IC50 = 112000 nM
|
[1] | |||
| Compound Name |
Chembl4225815
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461287
Click to Show/Hide
|
||||
| Activity |
IC50 = 153000 nM
|
[1] | |||
| Compound Name |
Chembl4224756
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461302
Click to Show/Hide
|
||||
| Activity |
IC50 = 165000 nM
|
[1] | |||
| Compound Name |
Chembl4225787
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461299
Click to Show/Hide
|
||||
| Activity |
IC50 = 166000 nM
|
[1] | |||
| Compound Name |
Chembl4224750
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461279
Click to Show/Hide
|
||||
| Activity |
IC50 = 171000 nM
|
[1] | |||
| Compound Name |
Chembl4225288
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461293
Click to Show/Hide
|
||||
| Activity |
IC50 = 195000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 19 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Chembl4226080
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461304
Click to Show/Hide
|
||||
| Activity |
IC50 = 212000 nM
|
[1] | |||
| Compound Name |
Chembl4225757
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461283
Click to Show/Hide
|
||||
| Activity |
IC50 = 239000 nM
|
[1] | |||
| Compound Name |
Chembl4226078
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461294
Click to Show/Hide
|
||||
| Activity |
IC50 = 248000 nM
|
[1] | |||
| Compound Name |
Chembl4225354
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461300
Click to Show/Hide
|
||||
| Activity |
IC50 = 270000 nM
|
[1] | |||
| Compound Name |
Chembl4226136
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461281
Click to Show/Hide
|
||||
| Activity |
IC50 = 288000 nM
|
[1] | |||
| Compound Name |
Chembl4224809
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461277
Click to Show/Hide
|
||||
| Activity |
IC50 = 300000 nM
|
[1] | |||
| Compound Name |
Chembl4225014
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461280
Click to Show/Hide
|
||||
| Activity |
IC50 = 319000 nM
|
[1] | |||
| Compound Name |
Chembl4229102
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461303
Click to Show/Hide
|
||||
| Activity |
IC50 = 326000 nM
|
[1] | |||
| Compound Name |
Chembl4226597
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461284
Click to Show/Hide
|
||||
| Activity |
IC50 = 328000 nM
|
[1] | |||
| Compound Name |
Chembl4226327
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461295
Click to Show/Hide
|
||||
| Activity |
IC50 = 332000 nM
|
[1] | |||
| Compound Name |
6-[({1-[2-(7-Methoxy-2-oxoquinoxalin-1(2H)-yl)ethyl]piperidin-4-yl}amino)methyl]-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL2165063; SCHEMBL708423; BDBM50395399
Click to Show/Hide
|
||||
| Activity |
IC50 > 333000 nM
|
[2] | |||
| Compound Name |
1-[(2S)-2-Amino-2-[(1r,4S)-4-[({3-oxo-2H,3H,4H-pyrido[3,2-b][1,4]oxazin-6-yl}methyl)amino]cyclohexyl]ethyl]-7-methoxy-1,2-dihydro-1,5-naphthyridin-2-one
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3355575; SCHEMBL1375971; SCHEMBL1375976; BDBM50023582; SB19210
Click to Show/Hide
|
||||
| Activity |
IC50 > 333000 nM
|
[2] | |||
| Compound Name |
Chembl4226924
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461275
Click to Show/Hide
|
||||
| Activity |
IC50 = 492000 nM
|
[1] | |||
| Compound Name |
Chembl4225492
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461285
Click to Show/Hide
|
||||
| Activity |
IC50 = 498000 nM
|
[1] | |||
| Compound Name |
Chembl4225227
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461291
Click to Show/Hide
|
||||
| Activity |
IC50 = 521000 nM
|
[1] | |||
| Compound Name |
Chembl4228579
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461298
Click to Show/Hide
|
||||
| Activity |
IC50 = 688000 nM
|
[1] | |||
| Compound Name |
Chembl4224963
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461286
Click to Show/Hide
|
||||
| Activity |
IC50 = 771000 nM
|
[1] | |||
| Compound Name |
Chembl4228834
Click to Show/Hide
|
Investigative | Compound Info | ||
| Activity |
IC50 > 1000000 nM
|
[1] | |||
| Compound Name |
Chembl4226804
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
BDBM50461288
Click to Show/Hide
|
||||
| Activity |
IC50 > 1000000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and evaluation of aminobenzothiazoles as blockers of N- and T-type calcium channels. Bioorg Med Chem. 2018 Jul 15;26(11):3046-3059. | ||||
| REF 2 | Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa. Bioorg Med Chem. 2014 Oct 1;22(19):5392-409. | ||||
| REF 3 | Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. J Med Chem. 2017 Jun 22;60(12):5072-5085. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.