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Compound Detail

CHEMBL3236549

JNJ-39758979
🧪 Phase II
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🧪 Phase II
CC(C)c1cc(N2CC[C@@H](N)C2)nc(N)n1

Basic Information

ChEMBL ID CHEMBL3236549
Name JNJ-39758979
Phase Phase II
Structure Type MOL
InChI Key COOGVHJHSCBOQT-MRVPVSSYSA-N

Known Names

Jnj 39758979 Jnj-39758979 JNJ-39758979, (-)- JNJ39758979
6
Targets
19
Activities
3
Assay Types
30
PK Parameters
20
Publications
4
Known Names
2
Indications

Molecular Properties

221.3
MW (Da)
0.72
ALogP
5
HBA
2
HBD
81.1
PSA (Ų)
0.77
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer

Flags

Chemical Probe

Extended Properties

Molecular Formula C11H19N5
MW 221.31
Aromatic Rings 1
Heavy Atoms 16
NP-Likeness -1.18

Indications

Arthritis, Rheumatoid Asthma

Activity Summary

Ki 13 meas. best 8.28
Kd 5 meas. best 8.3
IC50 1 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H4 receptor
CHEMBL5657
Kd 8.3 8.3 5.0 1
Histamine H4 receptor
CHEMBL5657
Ki 8.28 8.28 5.3 2
Histamine H4 receptor
CHEMBL5657
IC50 8.1 8.1 8.0 1
Histamine H4 receptor
CHEMBL3759
Ki 7.92 7.91 12.0 4
Histamine H4 receptor
CHEMBL3759
Kd 7.9 7.9 12.6 2
Unchecked
CHEMBL612545
Ki 7.6 7.6 25.0 2
Unchecked
CHEMBL612545
Kd 7.5 7.5 31.6 1
Histamine H4 receptor
CHEMBL4468
Kd 7.2 7.2 63.1 1
Histamine H4 receptor
CHEMBL4468
Ki 6.73 6.73 188.0 2
Histamine H4 receptor
CHEMBL1255160
Ki 6.51 6.51 306.0 2
Histamine H3 receptor
CHEMBL264
Ki 5.98 5.98 1043.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 309.83 ng.hr.mL-1 Rattus norvegicus
AUC 723.68 ng.hr.mL-1 Mus musculus
AUC 2144.49 ng.hr.mL-1 Mus musculus
AUC 5444.23 ng.hr.mL-1 Mus musculus
AUC 309.83 ng.hr.mL-1 Rattus norvegicus
AUC 537.78 ng.hr.mL-1 Rattus norvegicus
AUC 2963.34 ng.hr.mL-1 Rattus norvegicus
AUC 15768.34 ng.hr.mL-1 Rattus norvegicus
AUC 40754.24 ng.hr.mL-1 Rattus norvegicus
AUC 1482.78 ng.hr.mL-1 Canis lupus familiaris
AUC 6993.4 ng.hr.mL-1 Canis lupus familiaris
CL 2.2 L/hr Rattus norvegicus
CL 40.0 mL.min-1.kg-1 Mus musculus
CL 91.67 mL.min-1.kg-1 Rattus norvegicus
CL 23.33 mL.min-1.kg-1 Canis lupus familiaris
Cmax 300.0 nM Rattus norvegicus
Cmax 790.0 nM Mus musculus
Cmax 5030.0 nM Mus musculus
Cmax 260.0 nM Rattus norvegicus
Cmax 1250.0 nM Rattus norvegicus
Cmax 4910.0 nM Rattus norvegicus
Cmax 7070.0 nM Rattus norvegicus
Cmax 3900.0 nM Canis lupus familiaris
F 36.0 % Rattus norvegicus
F 84.0 % Mus musculus
F 75.0 % Mus musculus
F 35.0 % Rattus norvegicus
F 38.0 % Rattus norvegicus
F 51.0 % Rattus norvegicus
F 53.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histamine H4 receptor Kd = 5.012 nM 8.3 Antagonist activity at mouse histamine H4 receptor expressed in SK-N-MC cells as... 24495018
Histamine H4 receptor Ki = 5.3 nM 8.28 Displacement of [3H]histamine from mouse recombinant histamine H4 receptor 25993395
Histamine H4 receptor Ki = 5.3 nM 8.28 Displacement of [3H]histamine from mouse histamine H4 receptor expressed in SK-N... 24495018
Histamine H4 receptor IC50 = 8.0 nM 8.1 mBMMC chemotaxis -
Histamine H4 receptor Ki = 12.0 nM 7.92 Displacement of [3H]histamine from human recombinant histamine H4 receptor 25993395
Histamine H4 receptor Ki = 12.0 nM 7.92 Displacement of [3H]histamine from human recombinant histamine H4 receptor 25595684
Histamine H4 receptor Kd = 12.59 nM 7.9 Cell based cAMP Assays (pA2) -
Histamine H4 receptor Kd = 12.59 nM 7.9 Antagonist activity at human histamine H4 receptor expressed in SK-N-MC cells as... 24495018
Histamine H4 receptor Ki = 12.5 nM 7.9 Displacement of [3H]histamine from human recombinant histamine H4 receptor expre... 24495018
Histamine H4 receptor Ki = 12.5 nM 7.9 Binding assay -
Unchecked Ki = 25.0 nM 7.6 Binding affinity to monkey histamine H4 receptor 24495018
Unchecked Ki = 25.0 nM 7.6 Displacement of [3H]histamine from monkey recombinant histamine H4 receptor 25993395
Unchecked Kd = 31.62 nM 7.5 Antagonist activity at monkey histamine H4 receptor 24495018
Histamine H4 receptor Kd = 63.1 nM 7.2 Antagonist activity at rat histamine H4 receptor expressed in SK-N-MC cells asse... 24495018
Histamine H4 receptor Ki = 188.0 nM 6.73 Displacement of [3H]histamine from rat histamine H4 receptor expressed in SK-N-M... 24495018
Histamine H4 receptor Ki = 188.0 nM 6.73 Displacement of [3H]histamine from rat recombinant histamine H4 receptor 25993395
Histamine H4 receptor Ki = 306.0 nM 6.51 Binding affinity to guinea pig histamine H4 receptor 24495018
Histamine H4 receptor Ki = 306.0 nM 6.51 Displacement of [3H]histamine from guinea pig recombinant histamine H4 receptor 25993395
Histamine H3 receptor Ki = 1043.0 nM 5.98 Displacement of [3H]N-alpha-methylhistamine from human recombinant histamine H3 ... 24495018

Literature References

PubMed DOI Target Context # Activities
24495018 10.1021/jm401727m Rattus norvegicus 31
24495018 10.1021/jm401727m Mus musculus 17
- 10.6019/CHEMBL5058644 Unchecked 14
24495018 10.1021/jm401727m Canis familiaris 9
24495018 10.1021/jm401727m Histamine H4 receptor 8
24495018 10.1021/jm401727m ADMET 6
24495018 10.1021/jm401727m Plasma 6
25993395 10.1021/acs.jmedchem.5b00516 Histamine H4 receptor 4
24495018 10.1021/jm401727m Voltage-gated inwardly rectifying potassium channel KCNH2 3
24495018 10.1021/jm401727m Unchecked 3
24495018 10.1021/jm401727m Nucleic Acid 3
- 10.6019/CHEMBL5058644 Histamine H4 receptor 3
24495018 10.1021/jm401727m Liver microsome 3
- 10.6019/CHEMBL5058644 Muscarinic acetylcholine receptor M3 2
25993395 10.1021/acs.jmedchem.5b00516 Unchecked 2
24495018 10.1021/jm401727m Brain 2
24495018 10.1021/jm401727m Liver 2
24495018 10.1021/jm401727m Kidney 2
- 10.6019/CHEMBL5058644 Muscarinic acetylcholine receptor M1 2
- 10.6019/CHEMBL5058644 Muscarinic acetylcholine receptor M2 2

Data from ChEMBL 36 via Core Engine