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Compound Detail

CHEMBL1213158

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O=C(NCCO[C@@H]1[C@H](O)[C@@H](OP(=O)(O)O)[C@H](OP(=O)(O)O)[C@@H](O)[C@@H]1OP(=O)(O)O)NCCO[C@@H]1[C@H](O)[C@@H](OP(=O)(O)O)[C@H](O[PH](O)(O)O)[C@@H](O)[C@@H]1OP(=O)(O)O

Basic Information

ChEMBL ID CHEMBL1213158
Phase Preclinical
Structure Type MOL
InChI Key VZXIHMMJDSBIEQ-LHSKIUOISA-N
1
Targets
13
Activities
2
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

954.3
MW (Da)
-7.31
ALogP
21
HBA
19
HBD
544.2
PSA (Ų)
0.04
QED
3
Ro5 Violations
20
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H40N2O31P6
MW 954.33
Aromatic Rings 0
Heavy Atoms 56
NP-Likeness 0.11

Activity Summary

Kd 8 meas. best 9.74
EC50 5 meas. best 8.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1
CHEMBL2804
Kd 9.74 9.4025 0.2 8
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1
CHEMBL2804
EC50 8.57 8.026 2.7 5

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 Kd = 0.18 nM 9.74 Displacement of [3H]IP3 from rat recombinant IP3R1 binding core residue (224-604... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 Kd = 0.27 nM 9.57 Displacement of [3H]IP3 from rat recombinant IP3R1 N-terminal residue (1-604) V3... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 Kd = 0.32 nM 9.49 Displacement of [3H]IP3 from rat recombinant IP3R1 N-terminal residue (1-604) K1... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 Kd = 0.4 nM 9.4 Displacement of [3H]IP3 from rat recombinant IP3R1 N-terminal residue (1-604) R3... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 Kd = 0.41 nM 9.39 Displacement of [3H]IP3 from rat recombinant N-terminal IP3R1 (1-604) expressed ... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 Kd = 0.45 nM 9.35 Displacement of [3H]IP3 from full-length rat recombinant IP3R1 expressed in chic... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 Kd = 0.68 nM 9.17 Displacement of [3H]IP3 from rat recombinant IP3R1 N-terminal residue (1-604) D3... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 Kd = 0.78 nM 9.11 Displacement of [3H]IP3 from rat recombinant IP3R1 N-terminal residue (1-604) K5... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 EC50 = 2.7 nM 8.57 Agonist activity at rat recombinant IP3R1 expressed in chicken DT40 cells assess... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 EC50 = 7.7 nM 8.11 Agonist activity at rat recombinant IP3R1 K52E mutant expressed in chicken DT40 ... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 EC50 = 11.5 nM 7.94 Agonist activity at rat recombinant IP3R1 D34K mutant expressed in chicken DT40 ... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 EC50 = 15.8 nM 7.8 Agonist activity at rat recombinant IP3R1 R36E mutant expressed in chicken DT40 ... 19668195
Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 EC50 = 19.5 nM 7.71 Agonist activity at rat recombinant IP3R1 V33K mutant expressed in chicken DT40 ... 19668195

Literature References

PubMed DOI Target Context # Activities
19668195 10.1038/nchembio.195 Inositol 1,4,5-trisphosphate-gated calcium channel ITPR1 20

Data from ChEMBL 36 via Core Engine