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Compound Detail

CHEMBL52606

COLFORSIN
🧪 Phase II
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🧪 Phase II
C=C[C@@]1(C)CC(=O)[C@]2(O)[C@@]3(C)[C@@H](O)CCC(C)(C)[C@@H]3[C@H](O)[C@H](OC(C)=O)[C@@]2(C)O1

Basic Information

ChEMBL ID CHEMBL52606
Name COLFORSIN
Phase Phase II
Structure Type MOL
InChI Key OHCQJHSOBUTRHG-KGGHGJDLSA-N

Known Names

Boforsin Colforsin Colforsina Colforsine Forskolin HL 362 HL-362 L 75 1362B L-75-1362B L-751362B NSC-357088 NSC-375489
15
Targets
22
Activities
4
Assay Types
0
PK Parameters
20
Publications
12
Known Names

Molecular Properties

410.5
MW (Da)
1.52
ALogP
7
HBA
3
HBD
113.3
PSA (Ų)
0.47
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer

Flags

Natural Product
USAN Year 1986

Extended Properties

Molecular Formula C22H34O7
MW 410.51
Aromatic Rings 0
Heavy Atoms 29
NP-Likeness 3.14

Activity Summary

EC50 13 meas. best 7.33
IC50 6 meas. best 7.39
Kd 2 meas. best 7.54
Ki 1 meas. best 7.53

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Adenylate cyclase type 1
CHEMBL3549
Kd 7.54 7.54 29.0 1
Unchecked
CHEMBL612545
Ki 7.53 7.53 29.4 1
Adenylate cyclase type 1
CHEMBL2899
IC50 7.39 7.39 41.0 1
Relaxin receptor 1
CHEMBL1293316
EC50 7.33 7.33 47.0 1
Adenylate cyclase type 8
CHEMBL2960
EC50 7.03 7.03 93.7 1
Rattus norvegicus
CHEMBL376
EC50 6.62 6.62 240.0 1
Homo sapiens
CHEMBL372
EC50 6.62 6.62 240.0 2
Adenylate cyclase type 1
CHEMBL2899
EC50 6.3 6.3 500.0 1
Nuclear receptor subfamily 1 group I member 2
CHEMBL3401
EC50 6.16 5.42 700.0 4
Nuclear receptor subfamily 0 group B member 1
CHEMBL1795094
IC50 5.76 5.76 1729.0 1
Unchecked
CHEMBL612545
EC50 5.37 5.37 4300.0 1
Solute carrier family 2, facilitated glucose transporter member 1
CHEMBL2535
Kd 5.3 5.3 5000.0 1
Nuclear receptor subfamily 1 group I member 2
CHEMBL2146315
EC50 5.15 5.15 7100.0 1
SARS-CoV
CHEMBL4303836
EC50 5.12 5.12 7500.0 1
Sodium channel alpha subunits; brain (Types I, II, III)
CHEMBL2096682
IC50 4.22 4.22 60000.0 1
MCF7
CHEMBL387
IC50 4.2 4.2 63300.0 1
ATP-dependent translocase ABCB1
CHEMBL4302
IC50 4.1 4.1 80200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Adenylate cyclase type 1 Kd = 29.0 nM 7.54 Displacement of [125I]6-IHPP-Fsk from adenylate cyclase of bovine brain membrane 1956039
Unchecked Ki = 29.4 nM 7.53 Displacement of [3H]forskolin from forskolin site of adenylate cyclase 8496700
Adenylate cyclase type 1 IC50 = 41.0 nM 7.39 Inhibition of [125 I]6-IHPP-forskolin binding to adenylate cyclase 1 8709105
Relaxin receptor 1 EC50 = 47.0 nM 7.33 Agonist activity at human RXFP1 expressed in HEK293 cells assessed as increase i... 30006176
Adenylate cyclase type 8 EC50 = 93.7 nM 7.03 Agonist activity at recombinant human AC8 expressed in human HEK293 cells assess... 31776060
Homo sapiens EC50 = 240.0 nM 6.62 Compound was testd for inhibition of glucose transport human platelets using [H]... 10406641
Homo sapiens EC50 = 240.0 nM 6.62 Compound was testd for inhibition of glucose transport human erythrocytes using ... 10406641
Rattus norvegicus EC50 = 240.0 nM 6.62 Compound was tested for inhibition of glucose transport in adipocytes plasma mem... 10406641
Adenylate cyclase type 1 EC50 = 500.0 nM 6.3 Conversion of [32P] ATP to [32P]-cyclic AMP mediated by adenylate cyclase 1 8709105
Nuclear receptor subfamily 1 group I member 2 EC50 = 700.0 nM 6.16 Activation of PXR in human cryopreserved hepatocytes assessed as induction of CY... 20966043
Nuclear receptor subfamily 0 group B member 1 IC50 = 1729.0 nM 5.76 PubChem BioAssay. Luminescence-based cell-based high throughput dose response as... -
Nuclear receptor subfamily 1 group I member 2 EC50 = 2700.0 nM 5.57 Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induc... 20966043
Unchecked EC50 = 4300.0 nM 5.37 Stimulation of rat adenylate cyclase 20875743
Solute carrier family 2, facilitated glucose transporter member 1 Kd = 5000.0 nM 5.3 Inhibition of [125I]7-IHPP-Fsk binding to glucose transporter of human erythrocy... 1956039
Nuclear receptor subfamily 1 group I member 2 EC50 = 7100.0 nM 5.15 Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase ... 20966043
SARS-CoV EC50 = 7500.0 nM 5.12 Antiviral activity against SARS coronavirus in Vero E6 cells assessed as inhibit... 17663539
Nuclear receptor subfamily 1 group I member 2 EC50 = 7900.0 nM 5.1 Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by l... 20966043
Nuclear receptor subfamily 1 group I member 2 EC50 = 14100.0 nM 4.85 Competitive binding affinity to human PXR LBD (111 to 434) by TR-FRET assay 20966043
Sodium channel alpha subunits; brain (Types I, II, III) IC50 = 60000.0 nM 4.22 Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on vol... 2579237
MCF7 IC50 = 63300.0 nM 4.2 Antiproliferative activity against human MCF7 cells after 48 hrs by Alamar blue ... 28838692

Literature References

PubMed DOI Target Context # Activities
20966043 10.1124/dmd.110.035105 Nuclear receptor subfamily 1 group I member 2 9
19281221 10.1021/np800541k Skin 8
2849641 10.1021/np50059a019 Unchecked 6
- 10.6019/CHEMBL4495565 SARS-CoV-2 6
17663539 10.1021/jm070295s SARS-CoV 5
- 10.6019/CHEMBL4808148 Histone deacetylase 6 4
19966789 10.1038/nchembio.275 Histone deacetylase 7 4
12951096 10.1016/s0960-894x(03)00669-3 ADMET 4
8709105 10.1021/jm960191+ Adenylate cyclase type 1 4
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 3
11716514 10.1006/bbrc.2001.6000 ATP-dependent translocase ABCB1 3
- 10.6019/CHEMBL4651402 SARS-CoV-2 2
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 2
31776060 10.1016/j.bmcl.2019.126823 Adenylate cyclase type 8 2
2579237 10.1021/jm00381a019 Sodium channel alpha subunits; brain (Types I, II, III) 2
28838692 10.1016/j.bmcl.2017.08.033 MCF7 2
30481687 10.1016/j.ejmech.2018.10.006 Aquaporin-2 2
10406641 10.1016/s0960-894x(99)00270-x Homo sapiens 2
28448136 10.1021/acs.jnatprod.6b01086 Peroxisome proliferator-activated receptor gamma coactivator 1-alpha 2
11462981 10.1021/jm001059j 5-hydroxytryptamine receptor 1A 2

Data from ChEMBL 36 via Core Engine