Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL27266

INDOLACTUM
Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
CC(C)[C@H]1C(=O)N[C@H](CO)Cc2c[nH]c3cccc(c23)N1C
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL27266
Name INDOLACTUM
Phase Preclinical
Structure Type MOL
InChI Key LUZOFMGZMUZSSK-LRDDRELGSA-N
13
Targets
80
Activities
3
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

301.4
MW (Da)
1.66
ALogP
3
HBA
3
HBD
68.4
PSA (Ų)
0.79
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C17H23N3O2
MW 301.39
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness 1.52

Activity Summary

Ki 72 meas. best 8.7
EC50 5 meas. best 8.3
IC50 3 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein kinase C delta type
CHEMBL2560
 Ki 8.7 7.0773 2.0 15
RAS guanyl-releasing protein 1
CHEMBL3109
 Ki 8.6 8.6 2.5 1
HL-60
CHEMBL383
 EC50 8.3 8.3 5.0 1
Protein kinase C eta type
CHEMBL3616
 Ki 8.26 7.3133 5.5 6
Protein kinase C beta type
CHEMBL3045
 Ki 8.21 7.0363 6.1 8
Protein kinase C epsilon type
CHEMBL3582
 Ki 8.11 7.2686 7.7 7
Protein kinase C delta type
CHEMBL2996
 Ki 8.09 7.2867 8.2 9
Protein kinase C theta type
CHEMBL3920
 Ki 8.06 8.06 8.7 4
Protein kinase C alpha type
CHEMBL299
 Ki 7.96 6.9173 11.0 11
Unchecked
CHEMBL612545
 IC50 7.89 7.38 13.0 3
Protein kinase C gamma type
CHEMBL2938
 Ki 7.71 6.9533 19.4 9
Protein kinase C (PKC)
CHEMBL2093867
 EC50 7.33 6.885 47.0 2
Human immunodeficiency virus 1
CHEMBL378
 EC50 7.33 7.33 47.0 1
Unchecked
CHEMBL612545
 Ki 6.89 6.525 130.0 2
Unchecked
CHEMBL612545
 EC50 6.85 6.85 142.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein kinase C delta type Ki = 2.01 nM 8.7 Displacement of [3H]- PDBu from Protein kinase C delta C1b domain 11831896
Protein kinase C delta type Ki = 2.01 nM 8.7 Binding of Indolactam-V(ILV) to wild-type Protein kinase C delta C1b domain 10479277
Protein kinase C delta type Ki = 2.01 nM 8.7 Displacement of [3H]PDBu from protein kinase C delta C1b domain (Wild type) 11356104
RAS guanyl-releasing protein 1 Ki = 2.54 nM 8.6 Binding affinity against RAS guanyl releasing protein using [3H]- PDBu as the la... 11831896
HL-60 EC50 = 5.0 nM 8.3 Effective concentration against monocytes of HL-60 cells growth inhibition 9554881
Protein kinase C eta type Ki = 5.5 nM 8.26 Displacement of [3H]PDBu from PKCeta C1B domain 17977729
Protein kinase C eta type Ki = 5.5 nM 8.26 Displacement of [3H]PDBu from PKCeta C1B domain 18072722
Protein kinase C eta type Ki = 5.5 nM 8.26 Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C et... 11266178
Protein kinase C eta type Ki = 5.5 nM 8.26 Displacement of [3H]- PDBu from Protein kinase C eta C1b domain 10999477
Protein kinase C beta type Ki = 6.1 nM 8.21 Displacement of [3H]- PDBu from recombinant PKC beta expressed in baculovirus 9135029
Protein kinase C epsilon type Ki = 7.7 nM 8.11 Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C ep... 11266178
Protein kinase C epsilon type Ki = 7.7 nM 8.11 Displacement of [3H]- PDBu from Protein kinase C epsilon C1b domain 10999477
Protein kinase C epsilon type Ki = 7.7 nM 8.11 Displacement of [3H]PDBu from PKCepsilon C1B domain 17977729
Protein kinase C epsilon type Ki = 7.7 nM 8.11 Displacement of [3H]PDBu from PKCepsilon C1B domain 18072722
Protein kinase C delta type Ki = 8.2 nM 8.09 Displacement of [3H]- PDBu from recombinant PKC delta expressed in baculovirus 9135029
Protein kinase C delta type Ki = 8.3 nM 8.08 Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C de... 11266178
Protein kinase C delta type Ki = 8.3 nM 8.08 Displacement of [3H]- PDBu from Protein kinase C delta C1b domain 10999477
Protein kinase C theta type Ki = 8.7 nM 8.06 Inhibition of [3H]phorbol-12,13-dibutyrate (PDBu) binding to Protein kinase C th... 11266178
Protein kinase C theta type Ki = 8.7 nM 8.06 Displacement of [3H]PDBu from PKCtheta C1B domain 17977729
Protein kinase C theta type Ki = 8.7 nM 8.06 Displacement of [3H]- PDBu from Protein kinase C theta C1b domain 10999477

Literature References

PubMed DOI Target Context # Activities
19287398 10.1038/nchembio.154 Unchecked 49
10479277 10.1021/jm990129n Protein kinase C delta type 18
11356104 10.1021/jm000488e Protein kinase C delta type 18
30413535 10.1074/jbc.ra118.005798 Protein kinase C (PKC) 9
35859880 10.1021/acsmedchemlett.1c00562 Unchecked 7
11266178 10.1016/s0960-894x(01)00047-6 HL-60 6
- 10.1016/0960-894X(94)80010-3 HeLa 5
30413535 10.1074/jbc.ra118.005798 U1 5
30413535 10.1074/jbc.ra118.005798 ACH-2 cell line 5
18072722 10.1021/jm0706719 Unchecked 4
19287398 10.1038/nchembio.154 Intestine 3
11266178 10.1016/s0960-894x(01)00047-6 Protein kinase C delta type 3
30413535 10.1074/jbc.ra118.005798 ADMET 3
18072722 10.1021/jm0706719 Protein kinase C beta type 3
18072722 10.1021/jm0706719 Protein kinase C alpha type 3
30413535 10.1074/jbc.ra118.005798 J-Lat 6.3 3
18072722 10.1021/jm0706719 Protein kinase C gamma type 3
19287398 10.1038/nchembio.154 Molecular identity unknown 3
38036273 10.1016/j.bmcl.2023.129570 U-937 3
- 10.1016/0960-894X(95)00047-W Human gammaherpesvirus 4 3

Data from ChEMBL 36 via Core Engine