Compound Detail

CHEMBL3115681

NARAZACICLIB

🧪 Phase II

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🧪 Phase II

CN1CCN(c2ccc(Nc3ncc4cc(C#N)c(=O)n(C5CCCC5)c4n3)cc2)CC1

ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID	CHEMBL3115681
Name	NARAZACICLIB
Phase	Phase II
Structure Type	MOL
InChI Key	VADOZMZXXRBXNY-UHFFFAOYSA-N

Known Names

Narazaciclib On-123300 On123300

Targets

Activities

Assay Types

PK Parameters

Publications

Known Names

Indications

Molecular Properties

429.5

MW (Da)

3.27

ALogP

HBA

HBD

90.1

PSA (Å²)

0.68

QED

Ro5 Violations

Rot. Bonds

Drug Information

Molecule Type	Small molecule
Chirality	Achiral

USAN Stem

-ciclib

Extended Properties

Molecular Formula	C24H27N7O
MW	429.53
Aromatic Rings	3
Heavy Atoms	32
NP-Likeness	-1.57

Indications

Neoplasms Carcinoma, Endometrioid

Activity Summary

IC50 26 meas. best 8.42

Target Activity Profile

Target	Type	Best pChEMBL	Mean pChEMBL	Best (nM)	# Data
Cyclin-dependent kinase 4/cyclin D1 CHEMBL1907601	IC50	8.42	8.1933	3.8	3
NUAK family SNF1-like kinase 1 CHEMBL5784	IC50	8.3	8.3	5.0	2
Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041	IC50	8.04	8.04	9.2	1
CDK6/cyclin D1 CHEMBL2111455	IC50	8.01	8.01	9.8	1
Macrophage colony-stimulating factor 1 receptor CHEMBL1844	IC50	8.0	8.0	10.0	1
Tyrosine-protein kinase Fyn CHEMBL1841	IC50	7.96	7.96	11.0	2
Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974	IC50	7.91	7.91	12.2	1
DU-145 CHEMBL613508	IC50	7.6	7.6	25.0	1
Platelet-derived growth factor receptor beta CHEMBL1913	IC50	7.58	7.58	26.0	2
Fibroblast growth factor receptor 1 CHEMBL3650	IC50	7.58	7.58	26.0	2
K562 CHEMBL385	IC50	7.3	7.3	50.0	1
Tyrosine-protein kinase ABL1 CHEMBL1862	IC50	7.27	7.27	53.3	1
CDK2/Cyclin A2 CHEMBL3038469	IC50	7.26	7.03	55.0	2
CDK9/cyclin T1 CHEMBL2111389	IC50	6.93	6.93	117.0	1
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform CHEMBL3130	IC50	6.84	6.84	144.0	1
Cyclin-dependent kinase 5/CDK5 activator 1 CHEMBL1907600	IC50	6.57	6.57	272.0	1
Cyclin-dependent kinase 2/cyclin E1 CHEMBL1907605	IC50	6.42	6.42	377.0	1
Cyclin-dependent kinase 1/cyclin B1 CHEMBL1907602	IC50	6.22	6.22	600.0	1
CDK7/Cyclin H/MNAT1 CHEMBL3038473	IC50	5.22	5.22	6000.0	1

Activity Data Samples

Top measurements by pChEMBL value

Target	Type	Rel.	Value	Units	pChEMBL	Assay	PubMed
Cyclin-dependent kinase 4/cyclin D1	IC50	=	3.8	nM	8.42	Inhibition of CDK4/cyclinD1 (unknown origin)	24417566
Cyclin-dependent kinase 4/cyclin D1	IC50	=	3.87	nM	8.41	Inhibition of CDK4/cyclinD1 (unknown origin) using retinoblastoma as substrate a...	24417566
NUAK family SNF1-like kinase 1	IC50	=	4.95	nM	8.3	Inhibition of ARK5 (unknown origin)	24417566
NUAK family SNF1-like kinase 1	IC50	=	4.95	nM	8.3	Inhibition of human NUAK1	33356242
Proto-oncogene tyrosine-protein kinase receptor Ret	IC50	=	9.2	nM	8.04	Inhibition of RET (unknown origin)	33356242
CDK6/cyclin D1	IC50	=	9.82	nM	8.01	Inhibition of CDK6/cyclinD1 (unknown origin)	24417566
Macrophage colony-stimulating factor 1 receptor	IC50	=	10.0	nM	8.0	Inhibition of FMS (unknown origin)	24417566
Tyrosine-protein kinase Fyn	IC50	=	11.09	nM	7.96	Inhibition of FYN (unknown origin)	24417566
Tyrosine-protein kinase Fyn	IC50	=	11.0	nM	7.96	Inhibition of FYN (unknown origin)	33356242
Receptor-type tyrosine-protein kinase FLT3	IC50	=	12.22	nM	7.91	Inhibition of FLT3 (unknown origin)	24417566
Cyclin-dependent kinase 4/cyclin D1	IC50	=	18.0	nM	7.75	Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculoviru...	30234987
DU-145	IC50	=	25.0	nM	7.6	Cytotoxicity against human DU145 cells after 96 hrs by Cell-Titer Blue assay	24417566
Platelet-derived growth factor receptor beta	IC50	=	26.0	nM	7.58	Inhibition of PDGFRbeta (unknown origin)	24417566
Platelet-derived growth factor receptor beta	IC50	=	26.0	nM	7.58	Inhibition of PDGFRb (unknown origin)	33356242
Fibroblast growth factor receptor 1	IC50	=	26.0	nM	7.58	Inhibition of FGFR1 (unknown origin)	33356242
Fibroblast growth factor receptor 1	IC50	=	26.0	nM	7.58	Inhibition of FGFR1 (unknown origin)	24417566
K562	IC50	=	50.0	nM	7.3	Cytotoxicity against human K562 cells after 96 hrs by Cell-Titer Blue assay	24417566
Tyrosine-protein kinase ABL1	IC50	=	53.32	nM	7.27	Inhibition of ABL (unknown origin)	24417566
CDK2/Cyclin A2	IC50	=	55.0	nM	7.26	Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichi...	30234987
CDK9/cyclin T1	IC50	=	117.0	nM	6.93	Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus...	30234987

Literature References

PubMed	DOI	Target Context	# Activities
24417566	10.1021/jm401073p	NON-PROTEIN TARGET	17
24417566	10.1021/jm401073p	MDA-MB-231	7
24417566	10.1021/jm401073p	MCF7	5
24417566	10.1021/jm401073p	Cyclin-dependent kinase 4/cyclin D1	4
24417566	10.1021/jm401073p	Mus musculus	3
30234987	10.1021/acs.jmedchem.8b00049	HCT-116	2
-	10.6019/CHEMBL4495565	SARS-CoV-2	2
24417566	10.1021/jm401073p	DU-145	2
24417566	10.1021/jm401073p	K562	2
-	10.6019/CHEMBL4808148	Histone deacetylase 6	2
24417566	10.1021/jm401073p	Jurkat	1
24417566	10.1021/jm401073p	COLO 205	1
33356242	10.1021/acs.jmedchem.0c00533	Platelet-derived growth factor receptor beta	1
24417566	10.1021/jm401073p	A549	1
24417566	10.1021/jm401073p	BT-474	1
24417566	10.1021/jm401073p	Raji	1
24417566	10.1021/jm401073p	NCI-H417	1
24417566	10.1021/jm401073p	Unchecked	1
24417566	10.1021/jm401073p	Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform	1
24417566	10.1021/jm401073p	A-431	1

Data from ChEMBL 36 via Core Engine