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Compound Detail

CHEMBL430266

CALYCULIN A
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COC[C@@H]([C@H](O)[C@H](O)C(=O)NCC[C@H](C)c1nc(/C=C/C[C@@H]2O[C@]3(C[C@@H](O)[C@@H]2C)O[C@H]([C@H](C[C@H](O)[C@H](C)[C@H](O)[C@H](C)/C=C(C)/C(C)=C/C=C/C(C)=C\C#N)OC)[C@H](OP(=O)(O)O)C3(C)C)co1)N(C)C

Basic Information

ChEMBL ID CHEMBL430266
Name CALYCULIN A
Phase Preclinical
Structure Type MOL
InChI Key FKAWLXNLHHIHLA-YCBIHMBMSA-N
8
Targets
20
Activities
1
Assay Types
0
PK Parameters
18
Publications
0
Known Names

Molecular Properties

1009.2
MW (Da)

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C50H81N4O15P
MW 1009.18

Activity Summary

IC50 20 meas. best 9.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein phosphatase 2A 56 kDa regulatory subunit alpha isoform
CHEMBL4763
IC50 9.89 9.89 0.1 1
Serine/threonine-protein phosphatase PP1-gamma catalytic subunit
CHEMBL4438
IC50 9.85 8.6367 0.1 6
Serine-threonine protein phosphatase 2A regulatory subunit
CHEMBL2669
IC50 9.7 8.8467 0.2 3
Unchecked
CHEMBL612545
IC50 9.7 9.2725 0.2 4
Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform
CHEMBL4703
IC50 9.6 9.6 0.2 1
Tyrosine-protein phosphatase non-receptor type 1
CHEMBL335
IC50 9.52 9.2467 0.3 3
Serine/threonine-protein phosphatase 5
CHEMBL3425389
IC50 8.52 8.52 3.0 1
Serine/threonine-protein phosphatase 6 catalytic subunit
CHEMBL4105731
IC50 8.0 8.0 10.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein phosphatase 2A 56 kDa regulatory subunit alpha isoform IC50 = 0.13 nM 9.89 Tested for inhibition of purified catalytic subunit of protein phosphatase-2A fr... -
Serine/threonine-protein phosphatase PP1-gamma catalytic subunit IC50 = 0.14 nM 9.85 Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural to... 11881984
Serine-threonine protein phosphatase 2A regulatory subunit IC50 = 0.2 nM 9.7 Exogenous inhibition concentration of Serine/threonine protein phosphatase 2A (P... 11881984
Unchecked IC50 = 0.2 nM 9.7 Inhibition of PP4 (unknown origin) using [3H]-phosphohistone as substrate by liq... 34156850
Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform IC50 = 0.25 nM 9.6 Inhibition of human PP2AC using [3H]-phosphohistone as substrate 34156850
Unchecked IC50 = 0.3 nM 9.52 Exogenous inhibition of Serine/threonine protein phosphatase 1 (PP1) 11881984
Tyrosine-protein phosphatase non-receptor type 1 IC50 = 0.3 nM 9.52 Tested for inhibition against purified catalytic subunit of protein phosphatase-... -
Serine/threonine-protein phosphatase PP1-gamma catalytic subunit IC50 = 0.4 nM 9.4 Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural to... 11881984
Serine/threonine-protein phosphatase PP1-gamma catalytic subunit IC50 = 0.45 nM 9.35 Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural to... 11881984
Tyrosine-protein phosphatase non-receptor type 1 IC50 = 0.5 nM 9.3 Inhibitory concentration against Protein phosphatase 1 was determined; 0.5-1.0 11814804
Unchecked IC50 = 0.9 nM 9.05 Inhibition of protein phosphatase 2A 1812209
Tyrosine-protein phosphatase non-receptor type 1 IC50 = 1.2 nM 8.92 Observed inhibition activity of the compounds against protein phosphatases 1 (PP... 9379439
Unchecked IC50 = 1.5 nM 8.82 Inhibition of PP2A (unknown origin) using [3H]-phosphohistone as substrate by li... 34156850
Serine-threonine protein phosphatase 2A regulatory subunit IC50 = 2.0 nM 8.7 Concentration required to inhibit the action of protein phosphatase 2A 11814804
Serine/threonine-protein phosphatase PP1-gamma catalytic subunit IC50 = 2.2 nM 8.66 Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural to... 11881984
Serine/threonine-protein phosphatase 5 IC50 = 3.0 nM 8.52 Inhibition of human PP5 using [3H]-phosphohistone as substrate 34156850
Serine-threonine protein phosphatase 2A regulatory subunit IC50 = 7.3 nM 8.14 Observed inhibition activity of the compounds against protein phosphatases 2A (P... 9379439
Serine/threonine-protein phosphatase 6 catalytic subunit IC50 = 10.0 nM 8.0 Inhibition of PP6 (unknown origin) using [3H]-phosphohistone as substrate by liq... 34156850
Serine/threonine-protein phosphatase PP1-gamma catalytic subunit IC50 = 48.0 nM 7.32 Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural to... 11881984
Serine/threonine-protein phosphatase PP1-gamma catalytic subunit IC50 = 58.0 nM 7.24 Inhibition of Serine/threonine protein phosphatase 1 (PP1) mutants by natural to... 11881984

Literature References

PubMed DOI Target Context # Activities
11881984 10.1021/jm010066k Serine/threonine-protein phosphatase PP1-gamma catalytic subunit 10
11881984 10.1021/jm010066k Unchecked 4
34156850 10.1021/acs.jmedchem.1c00631 Unchecked 3
18622389 10.1038/nchembio.100 Saccharomyces cerevisiae 2
- 10.1016/S0960-894X(00)80281-4 Mus musculus 1
27784673 10.1182/blood-2016-08-731240 Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform 1
34156850 10.1021/acs.jmedchem.1c00631 Serine/threonine-protein phosphatase 6 catalytic subunit 1
34156850 10.1021/acs.jmedchem.1c00631 Serine/threonine-protein phosphatase 5 1
34156850 10.1021/acs.jmedchem.1c00631 Serine/threonine-protein phosphatase 2A catalytic subunit alpha isoform 1
12193024 10.1021/np020049d Spodoptera littoralis 1
1812209 10.1021/np50078a001 Unchecked 1
9379439 10.1021/jm960873x Serine-threonine protein phosphatase 2A regulatory subunit 1
- 10.1016/S0960-894X(00)80281-4 Serine/threonine-protein phosphatase 2A 56 kDa regulatory subunit alpha isoform 1
- 10.1016/S0960-894X(00)80281-4 Tyrosine-protein phosphatase non-receptor type 1 1
11881984 10.1021/jm010066k Serine-threonine protein phosphatase 2A regulatory subunit 1
11814804 10.1016/s0960-894x(01)00777-6 Serine-threonine protein phosphatase 2A regulatory subunit 1
11814804 10.1016/s0960-894x(01)00777-6 Tyrosine-protein phosphatase non-receptor type 1 1
9379439 10.1021/jm960873x Tyrosine-protein phosphatase non-receptor type 1 1

Data from ChEMBL 36 via Core Engine