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Compound Detail

CHEMBL313489

QUIFLAPON SODIUM
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CC(C)(C)Sc1c(CC(C)(C)C(=O)[O-])n(Cc2ccc(Cl)cc2)c2ccc(OCc3ccc4ccccc4n3)cc12.[Na+]

Basic Information

ChEMBL ID CHEMBL313489
Name QUIFLAPON SODIUM
Phase Preclinical
Structure Type MOL
InChI Key YPURUCMVRRNPHJ-UHFFFAOYSA-M
Parent Compound CHEMBL16596
Active Moiety CHEMBL16596

Known Names

MK-591 Quiflapon sodium
6
Targets
16
Activities
1
Assay Types
1
PK Parameters
8
Publications
2
Known Names

Molecular Properties

587.2
MW (Da)
9.01
ALogP
5
HBA
1
HBD
64.3
PSA (Ų)
0.17
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Achiral
USAN Stem -flapon
USAN Year 1995

Extended Properties

Molecular Formula C34H34ClN2NaO3S
MW 609.17
Aromatic Rings 5
Heavy Atoms 41
NP-Likeness -0.56

Activity Summary

IC50 16 meas. best 9.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Arachidonate 5-lipoxygenase-activating protein
CHEMBL4550
IC50 9.3 7.94 0.5 9
Rattus norvegicus
CHEMBL376
IC50 8.8 8.8 1.6 1
Homo sapiens
CHEMBL372
IC50 8.52 7.405 3.0 2
RBL-1
CHEMBL614772
IC50 8.22 8.22 6.0 1
Polyunsaturated fatty acid 5-lipoxygenase
CHEMBL215
IC50 8.1 8.1 8.0 1
Arachidonate 5-lipoxygenase-activating protein
CHEMBL1921661
IC50 8.0 7.465 10.0 2

Pharmacokinetic Data

Parameter Value Units Species
T1/2 6.0 hr -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Arachidonate 5-lipoxygenase-activating protein IC50 = 0.5 nM 9.3 Inhibition of FLAP in human peripheral leukocytes assessed as inhibition of calc... 22059882
Arachidonate 5-lipoxygenase-activating protein IC50 = 1.0 nM 9.0 Inhibition of FLAP in human peripheral leukocytes assessed as inhibition of calc... 22059882
Arachidonate 5-lipoxygenase-activating protein IC50 = 1.0 nM 9.0 Inhibition of FLAP in human peripheral leukocytes assessed as inhibition of calc... 22059882
Rattus norvegicus IC50 = 1.6 nM 8.8 Compound was tested for in vivo inhibition using FLAP binding assay 8709092
Arachidonate 5-lipoxygenase-activating protein IC50 = 1.9 nM 8.72 Displacement of [3H]-3-[5-(pyrid-2-ylmethoxy)-3-tert-butylthio-1-benzylindol-2-y... 22059882
Homo sapiens IC50 = 3.0 nM 8.52 Compound were tested for in vitro inhibition against human PMNL. 8709092
RBL-1 IC50 = 6.0 nM 8.22 Compound were tested for in vitro inhibition against broken RBL-1. 8709092
Polyunsaturated fatty acid 5-lipoxygenase IC50 = 8.0 nM 8.1 Inhibition of calcium ionophore (A-23187)-stimulated LTB4 formation in human neu... 10691695
Arachidonate 5-lipoxygenase-activating protein IC50 = 10.0 nM 8.0 Inhibition of FLAP in rat whole blood assessed as inhibition of calcium ionophor... 22059882
Arachidonate 5-lipoxygenase-activating protein IC50 = 12.0 nM 7.92 Inhibition of FLAP in human peripheral leukocytes assessed as inhibition of calc... 22059882
Arachidonate 5-lipoxygenase-activating protein IC50 = 66.0 nM 7.18 Inhibition of FLAP in human peripheral leukocytes assessed as inhibition of calc... 22059882
Arachidonate 5-lipoxygenase-activating protein IC50 = 80.0 nM 7.1 Inhibition of FLAP in human whole blood assessed as inhibition of calcium ionoph... 22059882
Arachidonate 5-lipoxygenase-activating protein IC50 = 108.0 nM 6.97 Inhibition of FLAP in human whole blood assessed as inhibition of calcium ionoph... 22059882
Arachidonate 5-lipoxygenase-activating protein IC50 = 117.0 nM 6.93 Inhibition of FLAP in rat whole blood assessed as inhibition of calcium ionophor... 22059882
Homo sapiens IC50 = 510.0 nM 6.29 Compound were tested for in vitro inhibition against human whole blood. 8709092
Arachidonate 5-lipoxygenase-activating protein IC50 = 536.0 nM 6.27 Inhibition of FLAP in human whole blood assessed as inhibition of calcium ionoph... 22059882

Literature References

PubMed DOI Target Context # Activities
22059882 10.1021/jm2008369 Arachidonate 5-lipoxygenase-activating protein 11
8709092 10.1021/jm960088k Homo sapiens 2
8709092 10.1021/jm960088k Unchecked 2
8709092 10.1021/jm960088k RBL-1 1
8709092 10.1021/jm960088k Rattus norvegicus 1
8709092 10.1021/jm960088k ADMET 1
10691695 10.1021/jm9904102 Polyunsaturated fatty acid 5-lipoxygenase 1
10691695 10.1021/jm9904102 Rattus norvegicus 1

Data from ChEMBL 36 via Core Engine