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Compound Detail

CHEMBL5567377

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CC[C@H](C)[C@H](NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H]([C@@H](C)O)C(=O)N1)[C@@H](C)O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](CC(N)=O)C(=O)N[C@H](C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O)[C@@H](C)O)C(C)C)[C@@H](C)O

Basic Information

ChEMBL ID CHEMBL5567377
Phase Preclinical
Structure Type MOL
InChI Key LIZHNINWBCQRGY-QJMUSDNHSA-N
7
Targets
13
Activities
2
Assay Types
5
PK Parameters
12
Publications
0
Known Names

Molecular Properties

3970.4
MW (Da)

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C168H266N54O54S2
MW 3970.43

Activity Summary

EC50 9 meas. best 10.24
IC50 4 meas. best 9.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Amylin receptor AMY1, CALCR/RAMP1
CHEMBL2111189
EC50 10.24 10.24 0.1 1
Amylin receptor AMY3; CALCR/RAMP3
CHEMBL2111190
EC50 10.12 9.935 0.1 2
Amylin receptor AMY2; CALCR/RAMP2
CHEMBL2364173
EC50 9.74 9.74 0.2 1
Amylin receptor AMY3; CALCR/RAMP3
CHEMBL2109235
EC50 9.58 9.58 0.3 1
Amylin receptor AMY3; CALCR/RAMP3
CHEMBL2109235
IC50 9.54 9.54 0.3 1
Amylin receptor AMY3; CALCR/RAMP3
CHEMBL2111190
IC50 9.25 9.25 0.6 1
Calcitonin receptor
CHEMBL1832
EC50 8.76 8.52 1.7 2
Calcitonin receptor
CHEMBL1832
IC50 7.38 7.38 42.0 1
Calcitonin receptor
CHEMBL2204
EC50 6.99 6.99 102.5 1
Calcitonin receptor
CHEMBL2204
IC50 6.87 6.87 135.0 1
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1
CHEMBL2107838
EC50 6.57 6.57 269.1 1

Pharmacokinetic Data

Parameter Value Units Species
F 40.0 % Rattus norvegicus
T1/2 24.0 hr Rattus norvegicus
T1/2 50.0 hr Oryctolagus cuniculus
T1/2 115.0 hr Sus scrofa
T1/2 76.0 hr Canis lupus familiaris

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Amylin receptor AMY1, CALCR/RAMP1 EC50 = 0.05754 nM 10.24 Agonist activity at human AMY1R complex of CTR/RAMP1 transduced in human HeLa ce... 38960379
Amylin receptor AMY3; CALCR/RAMP3 EC50 = 0.07586 nM 10.12 Agonist activity at human AMY3R complex of CTR/RAMP3 transduced in human HeLa ce... 38960379
Amylin receptor AMY3; CALCR/RAMP3 EC50 = 0.177 nM 9.75 Agonist activity at human AMY3R complex of CTR/RAMP3 expressed in Baby hamster k... 38960379
Amylin receptor AMY2; CALCR/RAMP2 EC50 = 0.182 nM 9.74 Agonist activity at human AMY2R complex of CTR/RAMP2 transduced in human HeLa ce... 38960379
Amylin receptor AMY3; CALCR/RAMP3 EC50 = 0.262 nM 9.58 Agonist activity at rat AMY3R complex of CTR/RAMP3 expressed in Baby hamster kid... 38960379
Amylin receptor AMY3; CALCR/RAMP3 IC50 = 0.29 nM 9.54 Displacement of 125I-rat amylin from rat AMY3R complex of CTR/RAMP3 expressed in... 38960379
Amylin receptor AMY3; CALCR/RAMP3 IC50 = 0.561 nM 9.25 Displacement of 125I-rat amylin from human AMY3R complex of CTR/RAMP3 expressed ... 38960379
Calcitonin receptor EC50 = 1.738 nM 8.76 Agonist activity at human CTR transduced in human HeLa cells by cAMP assay 38960379
Calcitonin receptor EC50 = 5.21 nM 8.28 Agonist activity at human CTR expressed in Baby hamster kidney cells incubated f... 38960379
Calcitonin receptor IC50 = 42.05 nM 7.38 Displacement of 125I-Calcitonin from human CTR expressed in Baby hamster kidney ... 38960379
Calcitonin receptor EC50 = 102.5 nM 6.99 Agonist activity at rat CTR expressed in Baby hamster kidney cells incubated for... 38960379
Calcitonin receptor IC50 = 134.99 nM 6.87 Displacement of 125I-Calcitonin from rat CTR expressed in Baby hamster kidney ce... 38960379
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 EC50 = 269.15 nM 6.57 Agonist activity at human CGRPR complex of CRLR/RAMP1 transduced in human HeLa c... 38960379

Literature References

PubMed DOI Target Context # Activities
38960379 10.1021/acs.jmedchem.4c00022 Rattus norvegicus 18
38960379 10.1021/acs.jmedchem.4c00022 No relevant target 8
38960379 10.1021/acs.jmedchem.4c00022 ADMET 7
38960379 10.1021/acs.jmedchem.4c00022 Unchecked 6
38960379 10.1021/acs.jmedchem.4c00022 Amylin receptor AMY3; CALCR/RAMP3 5
38960379 10.1021/acs.jmedchem.4c00022 Calcitonin receptor 5
38960379 10.1021/acs.jmedchem.4c00022 Canis familiaris 4
38960379 10.1021/acs.jmedchem.4c00022 Amylin receptor AMY1, CALCR/RAMP1 1
38960379 10.1021/acs.jmedchem.4c00022 Amylin receptor AMY2; CALCR/RAMP2 1
38960379 10.1021/acs.jmedchem.4c00022 Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 1
38960379 10.1021/acs.jmedchem.4c00022 Adrenomedullin receptor AM1; CALCRL/RAMP2 1
38960379 10.1021/acs.jmedchem.4c00022 Adrenomedullin receptor, AM2; CALCRL/RAMP3 1

Data from ChEMBL 36 via Core Engine