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Compound Detail

CHEMBL4802163

NEZULCITINIB
🧪 Phase II
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🧪 Phase II
CCc1cc(O)ccc1-c1ccc2c(-c3nc4c([nH]3)C[C@@H](C(=O)N3CC(N(C)C)C3)N(C(C)C)C4)n[nH]c2c1

Basic Information

ChEMBL ID CHEMBL4802163
Name NEZULCITINIB
Phase Phase II
Structure Type MOL
InChI Key VQIIUJSNIKEMCK-MHZLTWQESA-N

Known Names

Nezulcitinib Td-0903 THRX-136377
4
Targets
16
Activities
2
Assay Types
0
PK Parameters
0
Publications
3
Known Names
3
Indications
1
Mechanisms

Molecular Properties

527.7
MW (Da)
3.80
ALogP
6
HBA
3
HBD
104.4
PSA (Ų)
0.35
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer
USAN Stem -tinib
USAN Year 2021

Extended Properties

Molecular Formula C30H37N7O2
MW 527.67
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.59

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Janus Kinase (JAK) inhibitor INHIBITOR Janus Kinase (JAK)

Indications

Acute Lung Injury COVID-19 Severe Acute Respiratory Syndrome

Activity Summary

Ki 15 meas. best 10.49
IC50 1 meas. best 8.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tyrosine-protein kinase JAK2
CHEMBL2971
Ki 10.49 10.49 0.0 4
Tyrosine-protein kinase JAK3
CHEMBL2148
Ki 10.2 10.2 0.1 4
Tyrosine-protein kinase JAK1
CHEMBL2835
Ki 10.2 10.2 0.1 4
Non-receptor tyrosine-protein kinase TYK2
CHEMBL3553
Ki 9.1 9.1 0.8 3
Non-receptor tyrosine-protein kinase TYK2
CHEMBL3553
IC50 8.6 8.6 2.5 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Tyrosine-protein kinase JAK2 Ki = 0.032 nM 10.49 Biochemical Kinase Assay: A panel of four LanthaScreen JAK biochemical assays (J... -
Tyrosine-protein kinase JAK2 Ki = 0.032 nM 10.49 Biochemical JAK Kinase Assays: A panel of four LanthaScreen JAK biochemical assa... -
Tyrosine-protein kinase JAK2 Ki = 0.032 nM 10.49 Biochemical JAK Kinase Assays: A panel of four LanthaScreen JAK biochemical assa... -
Tyrosine-protein kinase JAK2 Ki = 0.032 nM 10.49 LanthaScreen JAK Biochemical Assays (JAK1, 2, 3 and Tyk2): A panel of four Lanth... -
Tyrosine-protein kinase JAK1 Ki = 0.063 nM 10.2 Biochemical Kinase Assay: A panel of four LanthaScreen JAK biochemical assays (J... -
Tyrosine-protein kinase JAK3 Ki = 0.063 nM 10.2 Biochemical Kinase Assay: A panel of four LanthaScreen JAK biochemical assays (J... -
Tyrosine-protein kinase JAK1 Ki = 0.063 nM 10.2 Biochemical JAK Kinase Assays: A panel of four LanthaScreen JAK biochemical assa... -
Tyrosine-protein kinase JAK3 Ki = 0.063 nM 10.2 Biochemical JAK Kinase Assays: A panel of four LanthaScreen JAK biochemical assa... -
Tyrosine-protein kinase JAK1 Ki = 0.063 nM 10.2 Biochemical JAK Kinase Assays: A panel of four LanthaScreen JAK biochemical assa... -
Tyrosine-protein kinase JAK3 Ki = 0.063 nM 10.2 Biochemical JAK Kinase Assays: A panel of four LanthaScreen JAK biochemical assa... -
Tyrosine-protein kinase JAK1 Ki = 0.063 nM 10.2 LanthaScreen JAK Biochemical Assays (JAK1, 2, 3 and Tyk2): A panel of four Lanth... -
Tyrosine-protein kinase JAK3 Ki = 0.063 nM 10.2 LanthaScreen JAK Biochemical Assays (JAK1, 2, 3 and Tyk2): A panel of four Lanth... -
Non-receptor tyrosine-protein kinase TYK2 Ki = 0.794 nM 9.1 Biochemical JAK Kinase Assays: A panel of four LanthaScreen JAK biochemical assa... -
Non-receptor tyrosine-protein kinase TYK2 Ki = 0.794 nM 9.1 Biochemical JAK Kinase Assays: A panel of four LanthaScreen JAK biochemical assa... -
Non-receptor tyrosine-protein kinase TYK2 Ki = 0.794 nM 9.1 LanthaScreen JAK Biochemical Assays (JAK1, 2, 3 and Tyk2): A panel of four Lanth... -
Non-receptor tyrosine-protein kinase TYK2 IC50 = 2.51 nM 8.6 Biochemical Kinase Assay: A panel of four LanthaScreen JAK biochemical assays (J... -

Data from ChEMBL 36 via Core Engine