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Compound Detail

CHEMBL442494

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CSCC[C@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CO)C(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C)C(=O)NCC(=O)N[C@@H]1CSSC[C@@H](C(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H]([C@@H](C)O)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H](CCCCN)NC1=O

Basic Information

ChEMBL ID CHEMBL442494
Phase Preclinical
Structure Type BOTH
InChI Key GGYTXJNZMFRSLX-OKOIUDDXSA-N
6
Targets
52
Activities
3
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

3148.6
MW (Da)

Drug Information

Molecule Type Protein
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C137H207N41O39S3
MW 3148.61

Activity Summary

IC50 45 meas. best 8.96
Ki 5 meas. best 9.51
EC50 2 meas. best 9.74

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CHO-K1
CHEMBL614031
EC50 9.74 9.425 0.2 2
Somatostatin receptor type 2
CHEMBL1804
Ki 9.51 9.51 0.3 1
Somatostatin receptor type 5
CHEMBL1792
Ki 9.4 9.4 0.4 1
Somatostatin receptor type 3
CHEMBL2028
IC50 8.96 8.5422 1.1 9
Somatostatin receptor type 3
CHEMBL2028
Ki 8.89 8.89 1.3 1
Somatostatin receptor type 4
CHEMBL1853
IC50 8.8 8.6356 1.6 9
Somatostatin receptor type 1
CHEMBL1917
IC50 8.72 8.6056 1.9 9
Somatostatin receptor type 1
CHEMBL1917
Ki 8.72 8.72 1.9 1
Somatostatin receptor type 2
CHEMBL1804
IC50 8.7 8.5967 2.0 9
Somatostatin receptor type 5
CHEMBL1792
IC50 8.68 8.6044 2.1 9
Somatostatin receptor type 4
CHEMBL1853
Ki 8.27 8.27 5.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CHO-K1 EC50 = 0.18 nM 9.74 Concentration for inhibition of forskolin-stimulated cAMP accumulation in CCL39 ... 15658864
Somatostatin receptor type 2 Ki = 0.31 nM 9.51 Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-2 recepto... 11312929
Somatostatin receptor type 5 Ki = 0.4 nM 9.4 Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-5 recepto... 11312929
CHO-K1 EC50 = 0.77 nM 9.11 Concentration for inhibition of forskolin-stimulated cAMP accumulation in CCL39 ... 15658864
Somatostatin receptor type 3 IC50 = 1.1 nM 8.96 Binding affinity to human sst3 by in vitro receptor autoradiography assay 24900340
Somatostatin receptor type 3 Ki = 1.3 nM 8.89 Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-3 recepto... 11312929
Somatostatin receptor type 4 IC50 = 1.6 nM 8.8 Displacement of [125I]-[LTT] SIRF-28 from human SST4 receptor expressed in human... 20666484
Somatostatin receptor type 4 IC50 = 1.6 nM 8.8 Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst4 receptor 18210999
Somatostatin receptor type 3 IC50 = 1.7 nM 8.77 Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombin... 19067538
Somatostatin receptor type 1 Ki = 1.9 nM 8.72 Ability to displace [125 I]labelled Tyr11-somatostatin from human hsst-1 recepto... 11312929
Somatostatin receptor type 1 IC50 = 1.9 nM 8.72 Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombin... 19067538
Somatostatin receptor type 2 IC50 = 2.0 nM 8.7 Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombin... 19067538
Somatostatin receptor type 4 IC50 = 2.0 nM 8.7 Displacement of [125I]-[Leu8, DTrp22, Tyr25]-somatostatin-28 from human recombin... 19067538
Somatostatin receptor type 1 IC50 = 2.0 nM 8.7 Binding affinity to human sst1 by in vitro receptor autoradiography assay 24900340
Somatostatin receptor type 5 IC50 = 2.1 nM 8.68 Displacement of [125I](Leu8,D-Trp22,Tyr25)-SRIF28 from human sst5 receptor 18210999
Somatostatin receptor type 5 IC50 = 2.1 nM 8.68 Binding affinity to human sst5 by in vitro receptor autoradiography assay 24900340
Somatostatin receptor type 4 IC50 = 2.2 nM 8.66 Binding affinity to human sst4 by in vitro receptor autoradiography assay 24900340
Somatostatin receptor type 1 IC50 = 2.2 nM 8.66 Displacement of [125I]-[Leu8, DTrp22, Tyr25]SRIF28 from human sst1 receptor expr... 18410083
Somatostatin receptor type 1 IC50 = 2.3 nM 8.64 Displacement of [125I]-[LTT] SIRF-28 from human SST1 receptor expressed in CHO c... 20666484
Somatostatin receptor type 2 IC50 = 2.3 nM 8.64 Inhibition of [Leu8,D-Trp22,125I-Tyr25]SRIF-28 binding to human somatostatin rec... 15658864

Literature References

PubMed DOI Target Context # Activities
15658864 10.1021/jm049520l CHO-K1 4
18410083 10.1021/jm701445q Somatostatin receptor type 2 2
18543899 10.1021/jm701618q Somatostatin receptor type 2 2
19351180 10.1021/jm801314f Somatostatin receptor type 1 2
10522693 10.1016/s0960-894x(99)00477-1 Muscarinic acetylcholine receptor M1 2
10522693 10.1016/s0960-894x(99)00477-1 Muscarinic acetylcholine receptor M2 2
10522693 10.1016/s0960-894x(99)00477-1 Muscarinic acetylcholine receptor M3 2
15658864 10.1021/jm049520l Somatostatin receptor type 2 1
18210999 10.1021/jm070886i Somatostatin receptor type 4 1
18210999 10.1021/jm070886i Somatostatin receptor type 3 1
18210999 10.1021/jm070886i Somatostatin receptor type 1 1
15658864 10.1021/jm049520l Somatostatin receptor type 5 1
15658864 10.1021/jm049520l Somatostatin receptor type 4 1
15658864 10.1021/jm049520l Somatostatin receptor type 3 1
11312929 10.1021/jm0005048 Somatostatin receptor type 1 1
24900340 10.1021/ml200032v Somatostatin receptor type 1 1
11312929 10.1021/jm0005048 Somatostatin receptor 1
11312929 10.1021/jm0005048 Somatostatin receptor type 5 1
11312929 10.1021/jm0005048 Somatostatin receptor type 4 1
11312929 10.1021/jm0005048 Somatostatin receptor type 3 1

Data from ChEMBL 36 via Core Engine